Page last updated: 2024-11-08

trichostatin a

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Description

trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID444732
CHEBI ID46024
CHEBI ID93196
SCHEMBL ID675951
SCHEMBL ID19886
MeSH IDM0059711

Synonyms (97)

Synonym
HY-15144
2,4-heptadienamide, 7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-, (2e,4e,6r)-
TSA ,
(2e,4e,6r)-7-(4-dimethylaminophenyl)-4,6-dimethyl-7-oxo-hepta-2,4-dienehydroxamic acid
trichlostatin a
SGCTO-002
tricostatin a
trichostatin a
58880-19-6
(2e,4e,6r)-7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide
c17h22n2o3
2,4-heptadienamide, 7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxo-, (2e,4e,6r)-
3C10 ,
7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide
a-300-i
2,4-heptadienamide, 7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-, (2e,4e,6r)- (9ci)
trichostatin a from streptomyces sp.
antibiotic a-300
(r)-trichostatin a
2,4-heptadienamide, 7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-, [r-(e,e)]-
2,4-heptadienamide, 7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxo-
[r-(e,e)]-7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide
TSN ,
trichostatin a, >=98% (hplc), from streptomyces sp.
(2e,4e,6r)-7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide
CHEBI:46024 ,
NCGC_TSA
1C3R
DB04297
(2e,4e,6r)-7-(4-dimethylaminophenyl)-n-hydroxy-4,6-dimethyl-7-oxo-hepta-2,4-dienamide
NCGC00162453-01
NCGC00162453-02
NCGC00162453-03
dtxsid6037063 ,
trichostatin a (tsa) ,
LMPK01000055
trichostatin
HMS1990L09
BRD-K68202742-001-04-1
T2477
gnf-pf-1011 ,
trichostatin(s)
BRD-K68202742-001-05-8
HMS1362L09
HMS1792L09
A25618
NCGC00162453-05
NCGC00162453-04
TRICHOSTATIN-A - TSA
3x2s926l3z ,
unii-3x2s926l3z
nsc 311042
BCPP000035
trichostatin a,tsa
M02571
3F0R
CS-0499
S1045
AKOS015899840
gtpl7005
CCG-208681
CCG-208142
MLS006011095
smr004702883
SCHEMBL675951
SCHEMBL19886
2,4-heptadienamide, 7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxo-,(2e,4e,6r)-
vtr-297
trichostatin a [mi]
trichostatina
trichostatine a
Q-201864
bdbm50005711
7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6r-dimethyl-7-oxo-2e,4e-heptadienamide
(2e,4e,6r)-7-(4-(dimethylamino)phen yl)-n-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamid e
HB1402
(r,2e,4e)-7-(4-(dimethylamino)phenyl)-n-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide
HMS3403L09
HMS3649O20
mfcd03848392
CHEBI:93196
AS-74315
trichostatin a??, vetec(tm) reagent grade, from streptomyces sp., >=98%
NCGC00162453-15
SW219664-1
'7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide'
trichostatin-a
BCP01776
trichostatin a, streptomyces sp. - cas 58880-19-6
58880-19-6 (r-isomer)
EX-A1665
sr-05000013796
SR-05000013796-3
Q425894
2,4-heptadienamide,7-[4-(dimethylamino)phenyl]-n-hydroxy-4,6-dimethyl-7-oxo-, (2e,4e,6r)-
PD119680
AC-35470

Research Excerpts

Overview

Trichostatin A (TSA) is a novel histone deacetylase inhibitor (HDACI) that was recently reported to exert multiple pharmacological functions. It specifically inhibits the biochemical functions of HDAC and is demonstrated to be an active anticancer drug.

ExcerptReferenceRelevance
"Trichostatin A (TSA) is a novel histone deacetylase inhibitor (HDACI) that was recently reported to exert multiple pharmacological functions."( HDAC inhibitor Trichostatin A suppresses adipogenesis in 3T3-L1 preadipocytes.
Hao, T; Jiang, H; Lv, X; Qiu, J; Tan, Y; Zhang, H, 2021
)
1.7
"Trichostatin A (TSA) is a noncompetitive, reversible inhibitor of class I and II histone deacetylases (HDACs)."( The histone deacetylase class I, II inhibitor trichostatin A delays peripheral neurodegeneration.
Jung, J; Kim, M; Park, C; Yeo, SG, 2019
)
1.49
"Trichostatin A (TsA) is a pan-inhibitor of HDAC."( Trichostatin A Inhibits Rhabdomyosarcoma Proliferation and Induces Differentiation through MyomiR Reactivation.
Bujak, J; Kopytko, P; Pawlik, A; Piotrowska, K; Tarnowski, M; Tkacz, M, 2019
)
2.68
"Trichostatin A (TSA) is a classic histone deacetylases inhibitor (HDACi) that specifically inhibits the biochemical functions of HDAC and is demonstrated to be an active anticancer drug."( Inhibition of autophagy induced by TSA sensitizes colon cancer cell to radiation.
He, G; Pang, X; Wang, Y; Zhang, B, 2014
)
1.12
"Trichostatin A (TSA) is a selective inhibitor of mammalian histone deacetylase. "( Trichostatin A specifically stimulates gonadotropin FSHβ gene expression in gonadotroph LβT2 cells.
Kanasaki, H; Mijiddorj, T; Miyazaki, K; Oride, A; Sukhbaatar, U, 2014
)
3.29
"Trichostatin A (TSA) is a histone deacetylase (HDAC) inhibitor. "( Effect of trichostatin A on CNE2 nasopharyngeal carcinoma cells--genome-wide DNA methylation alteration.
Lina, X; Liu, XC; Lu, SM; Qin, MB; Wu, H; Wu, HY; Wu, YH; Yang, XL; Zhang, CD; Zhang, YN, 2014
)
2.25
"Trichostatin A (TSA) is a histone deacetylase inhibitor with beneficial effects in spinal muscular atrophy mouse models that carry the human SMN2 transgene."( The Smn-independent beneficial effects of trichostatin A on an intermediate mouse model of spinal muscular atrophy.
Beauvais, A; Kothary, R; Liu, H; Murray, LM; Yazdani, A, 2014
)
1.39
"Trichostatin A (TSA) is a kind of classical histone deacetylase (HDAC) inhibitor. "( Trichostatin A, a histone deacetylase inhibitor, reverses epithelial-mesenchymal transition in colorectal cancer SW480 and prostate cancer PC3 cells.
Cai, S; Du, J; Wang, H; Wang, X; Wu, L; Xu, J; Yuan, W, 2015
)
3.3
"Trichostatin A (TSA) is a histone deacetylase inhibitor with anti-inflammatory effects. "( Protection against reperfusion lung injury via aborgating multiple signaling cascades by trichostatin A.
Chu, SJ; Hsu, HH; Huang, KL; Li, MH; Tang, SE; Wu, GC; Wu, SY, 2015
)
2.08
"Trichostatin A (TSA) is an anti-inflammatory agent that has been shown to exert protective effects against cisplatin-induced ototoxicity."( Trichostatin A reduces cisplatin-induced ototoxicity through the STAT6 signaling pathway.
Chen, J; Chen, X; Ge, J; Huang, J; Li, M; Wang, P, 2015
)
2.58
"Trichostatin A (TSA) is a histone deacetylase inhibitor and a potential therapeutic for various malignancies. "( Trichostatin A suppresses lung adenocarcinoma development in Grg1 overexpressing transgenic mice.
Allen, TD; Dong, F; Li, L; Li, Y; Liu, J; Lobe, CG; Masuda, T, 2015
)
3.3
"Trichostatin A (TSA) is a selective inhibitor of mammalian histone deacetylase and is widely used to modify the ability of DNA transcription factors to bind DNA within chromatin by interfering with histone deacetylation. "( Trichostatin A reduces GnRH mRNA expression with a concomitant increase in retinaldehyde dehydrogenase in GnRH-producing neurons.
Ishihara, T; Kanasaki, H; Kyo, S; Mijiddorj, T; Oride, A; Sukhbaatar, U; Yamagami, I, 2015
)
3.3
"Trichostatin A (TSA) is a potent cell-permeable HDAC inhibitor that blocks cell cycle progression."( Inhibitory effects of trichostatin A on adrenocorticotropic hormone production and proliferation of corticotroph tumor AtT-20 cells.
Asari, Y; Daimon, M; Desaki, R; Ishigame, N; Iwasaki, Y; Kageyama, K; Murasawa, S; Nakada, Y; Niioka, K; Sugiyama, A; Takayasu, S, 2015
)
1.45
"Trichostatin A (TSA) is a well-known histone deacetylases (HDACs) inhibitor that has been reported to show potent anti-tumor capabilities in some types of cancer cell lines. "( PU.1-Bim axis is involved in Trichostatin A-induced apoptosis in murine pro-B lymphoma FL5.12 cells.
Li, C; Liu, B; Liu, H; Liu, J; Tao, Y; Wang, G, 2016
)
2.17
"Trichostatin A (TSA) is an HDAC inhibitor specific in class I and II HDAC enzymes."( Trichostatin A protects against intestinal injury in rats with acute liver failure.
Chu, XG; Gong, ZJ; Li, X; Wang, LW; Yang, F; Zhang, H; Zhang, HY; Zhang, Q, 2016
)
2.6
"Trichostatin A (TSA) is an inhibitor of histone deacetylase, potentially enhancing cloning efficiency."( High in vitro development after somatic cell nuclear transfer and trichostatin A treatment of reconstructed porcine embryos.
Bolund, L; Bøgh, IB; Du, Y; Kragh, PM; Li, J; Lin, L; Maddox-Hyttel, P; Purup, S; Schmidt, M; Svarcova, O; Vajta, G; Villemoes, K; Xue, Q; Yang, H; Zhang, Y, 2008
)
1.3
"Trichostatin A (TSA) is a histone deacetylase inhibitor that has antiproliferative and differentiation-inducing effects on cancer cells, and in cultures of primary hepatocytes has been shown to maintain xenobiotic metabolic capacity. "( Effect of the histone deacetylase inhibitor trichostatin a on the metabolome of cultured primary hepatocytes.
Athersuch, TJ; Cavill, R; Chan, PH; Doktorova, T; Ellis, JK; Keun, HC; M D Ebbels, T; Nicholson, JK; Rogiers, V; Vanhaecke, T; Vinken, M, 2010
)
2.06
"Trichostatin A (TSA) is a well-characterized histone deacetylase (HDAC) inhibitor. "( Trichostatin A enhances acetylation as well as protein stability of ERalpha through induction of p300 protein.
Kang, HJ; Kim, SH; Lee, MO; Na, H, 2010
)
3.25
"Trichostatin A (TSA) is a histone deacetylase inhibitor (HDACi) known to modulate differentiation of many cells. "( Trichostatin A inhibits TGF-β1 induced in vitro chondrogenesis of hMSCs through Sp1 suppression.
Chen, TH; Chen, YT; Chiang, ER; Hung, SC; Lee, HH; Lee, YT; Liu, CL; Wang, JP; Wen, MH, 2011
)
3.25
"Trichostatin A (TSA) is a histone deacetylase inhibitor that induces histone hyperacetylation and increases gene expression levels. "( Supplementation with the histone deacetylase inhibitor trichostatin A during in vitro culture of bovine embryos.
de Lima, MR; de Souza, MM; Garcia, JM; Oliveira, CS; Saraiva, NZ; Tetzner, Tde A, 2013
)
2.08
"Trichostatin A (TSA) is a most potent reversible inhibitor of mammalian histone deacetylases."( Cell-cycle-dependent variations in the FTIR spectroscopy of HeLa cells treated with trichostatin A.
Qi, J; Yang, ZG; Zhang, FQ, 2011
)
1.32
"Trichostatin A (TSA) is a potent histone deacetylase inhibitor and widely used as a promising anticancer agent. "( Trichostatin A ameliorates myocardial ischemia/reperfusion injury through inhibition of endoplasmic reticulum stress-induced apoptosis.
Chen, X; Lu, M; Wang, P; Yu, L, 2012
)
3.26
"Trichostatin A (TSA) is a potent histone deacetylase (HDAC) inhibitor with a broad spectrum of epigenetic activities known to regulate diverse cellular mechanisms, including differentiation of mesenchymal stem cells. "( HDAC inhibitor trichostatin A promotes proliferation and odontoblast differentiation of human dental pulp stem cells.
Choi, H; Choung, PH; Jin, H; Park, JY, 2013
)
2.19
"Trichostatin A (TSA) is a histone deacetylase (HDAC) inhibitor with potential in cancer therapeutics. "( Differential effects of trichostatin A on gelatinase A expression in 3T3 fibroblasts and HT-1080 fibrosarcoma cells: implications for use of TSA in cancer therapy.
Ailenberg, M; Silverman, M, 2003
)
2.07
"Trichostatin A is a potent and specific histone deacetylase inhibitor with promising antitumor activity in preclinical models. "( Plasma pharmacokinetics and metabolism of the histone deacetylase inhibitor trichostatin a after intraperitoneal administration to mice.
Aboagye, EO; Alao, JP; Coombes, RC; Latigo, JR; Sanderson, L; Taylor, GW; Vigushin, DM, 2004
)
2
"Trichostatin A (TSA) is a histone deacetylase inhibitor that causes growth inhibition of malignant cells. "( Effect of trichostatin A, a histone deacetylase inhibitor, on glioma proliferation in vitro by inducing cell cycle arrest and apoptosis.
Arnold, B; Pollack, IF; Premkumar, DR; Wetzel, M, 2005
)
2.17
"Trichostatin A (TSA) is a potent histone deacetylase inhibitor and has demonstrated significant antitumor activity against a variety of cancer cell lines. "( The efficacy of combination therapy using adeno-associated virus--interferon beta and trichostatin A in vitro and in a murine model of neuroblastoma.
Cutshaw, A; Davidoff, AM; Dickson, PV; Hamner, JB; McGee, M; Ng, CY; Rosati, S; Sims, TL, 2008
)
2.01
"Trichostatin A (TSA) is a Streptomyces metabolite which specifically inhibits mammalian histone deacetylase at a nanomolar concentration and causes accumulation of highly acetylated histone molecules in mammalian cells. "( Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines.
Beppu, T; Horinouchi, S; Hoshikawa, Y; Kwon, HJ; Yoshida, M, 1994
)
3.17
"Trichostatin A is a specific inhibitor of histone deacetylase; therefore, we propose that hyperacetylation of histones after drug treatment changes the structure of chromatin on integrated viral sequences and relieves repression of transduced genes."( Reactivation of silenced, virally transduced genes by inhibitors of histone deacetylase.
Bailey, EC; Chen, WY; Dong, JY; McCune, SL; Townes, TM, 1997
)
1.02
"Trichostatin A (TSA) is a potent reversible inhibitor of histone deacetylase, and it has been reported to have variable effects on the expression of a number of genes. "( Effect of trichostatin A on human T cells resembles signaling abnormalities in T cells of patients with systemic lupus erythematosus: a new mechanism for TCR zeta chain deficiency and abnormal signaling.
Fisher, CU; Nambiar, MP; Tsokos, GC; Warke, VG, 2002
)
2.16
"(R)-Trichostatin A (TSA) is a Streptomyces product which causes the induction of Friend cell differentiation and specific inhibition of the cell cycle of normal rat fibroblasts in the G1 and G2 phases at the very low concentrations. "( Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A.
Akita, M; Beppu, T; Kijima, M; Yoshida, M, 1990
)
1.06

Effects

Trichostatin A (TSA) has been revealed to show protective effect on central nervous systems in Alzheimer's disease (AD) and hypoxic-ischemic brain injury. TSA has been shown to mitigate whole body γ-radiation-induced morbidity and mortality.

ExcerptReferenceRelevance
"Trichostatin A (TSA) has been revealed to show protective effect on central nervous systems in Alzheimer's disease (AD) and hypoxic-ischemic brain injury."( Quantitative Proteomics Characterization of the Effect and Mechanism of Trichostatin A on the Hippocampus of Type II Diabetic Mice.
Hao, J; Jin, T; Kong, D; Li, F; Wei, W; Zhang, Q; Zhao, J; Zhao, S; Zhu, L, 2023
)
1.86
"Trichostatin A (TSA) has been shown to mitigate whole body γ-radiation-induced morbidity and mortality. "( Gut microbiota response to ionizing radiation and its modulation by HDAC inhibitor TSA.
Agrawala, PK; Gupta, N; Kainthola, A; Tiwari, M, 2020
)
2
"Trichostatin A (TSA) has previously been used in somatic cell nuclear transfer (SCNT) to improve the cloning efficiency in several species, which led our team to investigate the effects of TSA on the full-term development of bovine SCNT and gaur-bovine interspecies SCNT (gaur iSCNT; gaur somatic cells as donors and bovine oocytes as recipients) embryos. "( Full-term development of gaur-bovine interspecies somatic cell nuclear transfer embryos: effect of trichostatin A treatment.
Chaimongkol, C; Imsoonthornruksa, S; Ketudat-Cairns, M; Laowtammathron, C; Parnpai, R; Sangmalee, A; Srirattana, K; Thongprapai, T; Tunwattana, W, 2012
)
2.04
"Trichostatin A (TSA) has been shown to prevent fibrosis in vitro and in vivo. "( Trichostatin A inhibits transforming growth factor-β-induced reactive oxygen species accumulation and myofibroblast differentiation via enhanced NF-E2-related factor 2-antioxidant response element signaling.
Chen, P; Danielson, P; Duan, H; Qu, M; Shi, W; Wang, Y; Yang, L; Zhou, Q, 2013
)
3.28
"Trichostatin A (TSA) has potent antitumor activity, but its exact mechanism on EBV-infected cells is unclear."( Involvement of caspase activation and mitochondrial stress in trichostatin A-induced apoptosis of Burkitt's lymphoma cell line, Akata.
Choi, KC; Jang, YS; Jeon, YM; Kim, J; Kim, JG; Kook, SH; Lee, HJ; Lee, JC; Lee, WK; Son, YO, 2006
)
1.3

Actions

Trichostatin A (TSA) promotes SCNT embryo development, but whether TSA modifies SCNT blastocyst numbers is unclear. TSA was used to inhibit histone deacetylases (HDACs) TSA did not inhibit degradation of IκBα, nuclear translocation and DNA binding of NF-κB.

ExcerptReferenceRelevance
"Trichostatin A (TSA) promotes SCNT embryo development, but whether TSA modifies SCNT blastocyst numbers is unclear."( Effects of trichostatin A on pig SCNT blastocyst formation rate and cell number: A meta-analysis.
Fu, B; Guo, Z; Liu, D; Lv, L, 2018
)
1.59
"Trichostatin A was used to inhibit histone deacetylases (HDACs)."( Histone deacetylase inhibition disturbs the balance between ACE and chymase expression in endothelial cells: a potential mechanism of chymase activation in preeclampsia.
Alexander, JS; Gu, Y; Lewis, DF; Wang, Y, 2019
)
1.24
"Trichostatin A did not inhibit degradation of IκBα, nuclear translocation and DNA binding of NF-κB; also, the drug did not affect transient expression from exogenous κB-reporter plasmids."( Histone deacetylase inhibitors block nuclear factor-κB-dependent transcription by interfering with RNA polymerase II recruitment.
Furumai, R; Horinouchi, S; Ito, A; Maeda, S; Nishino, N; Ogawa, K; Saito, A; Yoshida, M, 2011
)
1.09

Treatment

Trichostatin A and ADC treatment also suppressed the cell cycle progression in ectopic endometrial stromal cells. The treatment also showed therapeutic effects on arthritis in SKG mice.

ExcerptReferenceRelevance
"Trichostatin A treatment remarkably suppressed osteogenesis, decreasing HDAC expression and enhancing histone H3 acetylation."( Regulation of osteogenesis in bone marrow-derived mesenchymal stem cells via histone deacetylase 1 and 2 co-cultured with human gingival fibroblasts and periodontal ligament cells.
Fujita, T; Ishida, S; Iwata, T; Kajiya, M; Kaneda-Ikeda, E; Kurihara, H; Matsuda, S; Mizuno, N; Nagahara, T; Ouhara, K; Sasaki, S; Takahashi, K; Takeda, K; Yoshioka, M, 2023
)
1.63
"Trichostatin A treatment induced CTNNA2 expression in SK-N-AS cells, and combination treatment with Trichostatin A induced retinoic acid sensitivity in retinoic acid-resistant cells."( Reactivation of silenced α-N-catenin induces retinoic acid sensitivity in neuroblastoma cells.
Chung, DH; Clark, RA; Lee, S; Newton, M; Qiao, J, 2021
)
1.34
"Trichostatin A treatment also resulted in cell stiffening and decreased migratory ability in KFs."( Caveolin-1 Controls Hyperresponsiveness to Mechanical Stimuli and Fibrogenesis-Associated RUNX2 Activation in Keloid Fibroblasts.
Chen, WR; Cheng, CM; Harn, HI; Ho, YT; Hsu, CK; Lee, JY; Lee, YC; Lin, HH; McGrath, JA; Ogawa, R; Shieh, SJ; Tang, MJ; Wang, YK, 2018
)
1.2
"Trichostatin A treatment resulted in an increase in MKK3 phosphorylation or acetylation in myocardium."( HDAC inhibition elicits myocardial protective effect through modulation of MKK3/Akt-1.
Du, J; Liu, P; Zhang, LX; Zhao, TC; Zhuang, S, 2013
)
1.11
"Trichostatin A treatment could moderately increase H3-K9 acetylation at the silenced loci; however, it had no effect on DNA and H3-K9 methylation and minimal effects on NGX6 expression."( DNA promoter and histone H3 methylation downregulate NGX6 in gastric cancer cells.
Dai, D; Liu, J; Xu, X; Zhu, X, 2014
)
1.12
"Trichostatin A treatment of donor cells significantly improved both cleavage and blastocyst rate (P<0.05) compared with the control embryos, also apoptotic index in treated cloned blastocysts was significantly decreased compared with the nontreated blastocysts (P<0.05) and was at the level of IVF counterpart."( Trichostatin A alters the expression of cell cycle controlling genes and microRNAs in donor cells and subsequently improves the yield and quality of cloned bovine embryos in vitro.
Chauhan, MS; Madan, P; Palta, P; Revey, T; Saini, M; Selokar, NL; Singla, SK, 2014
)
2.57
"Trichostatin A treatment of human epidermoid carcinoma A431 cells inhibited the EGF-induced 12(S)-lipoxygenase enzymatic activity in a dose-dependent manner that was consistent with the expression of 12(S)-lipoxygenase mRNA and protein."( Attenuation of c-Jun and Sp1 expression and p300 recruitment to gene promoter confers the trichostatin A-induced inhibition of 12(S)-lipoxygenase expression in EGF-treated A431 cells.
Chang, WC; Chen, BK; Chen, CJ, 2008
)
1.29
"Trichostatin A and ADC treatment also suppressed the cell cycle progression in ectopic endometrial stromal cells."( Promoter hypermethylation of progesterone receptor isoform B (PR-B) in adenomyosis and its rectification by a histone deacetylase inhibitor and a demethylation agent.
Guo, SW, 2010
)
1.08
"Trichostatin A treatment also showed therapeutic effects on arthritis in SKG mice, when it was administered after the onset of arthritis."( Histone deacetylase inhibition alters dendritic cells to assume a tolerogenic phenotype and ameliorates arthritis in SKG mice.
Fujita, M; Kasagi, S; Kumagai, S; Matsuki, F; Misaki, K; Miyamoto, Y; Morinobu, A; Saegusa, J, 2011
)
1.09
"Trichostatin A treatment results in not only histone hyperacetylation but also an increase in methylation of H3-K4, increase in dual modification of pS10/acK14, and reduction in methylation of H3-K9, revealing an extensive interplay between histone acetylation, methylation, and phosphorylation."( Involvement of histone methylation and phosphorylation in regulation of transcription by thyroid hormone receptor.
Allis, CD; Huang, ZQ; Li, J; Lin, Q; Strahl, BD; Wong, J; Yoon, HG, 2002
)
1.04
"Trichostatin A treatment reduced the percentage of cells in S phase (10% to 23%) and increased G1 populations (10% to 40%) as determined by flow cytometry."( Effectiveness of trichostatin A as a potential candidate for anticancer therapy in non-small-cell lung cancer.
Bueno, R; Gilchrist, D; Jaklitsch, MT; Mukhopadhyay, NK; Sugarbaker, DJ; Weisberg, E, 2006
)
1.39
"Trichostatin A treatment elevated expression of ADH1C."( Differential regulation of the alcohol dehydrogenase 1B (ADH1B) and ADH1C genes by DNA methylation and histone deacetylation.
Chen, HJ; Dannenberg, LO; Edenberg, HJ; Tian, H, 2006
)
1.06
"Trichostatin A treatment led to a time- and dose-dependent inhibition in carcinoma cells A549 proliferation (Twenty-four hours after the treatment of TSA The inhibition rates of the A549 cells in the control group and the cells treated with TSA of the concentrations of 5, 10, 20, and 40 microg/L were 6.2%+/-1.1%, 18.5%+/-2.3%, 28.9%+/-3.6%, 39.4%+/-3.7%, and 45.6%+/-2.7% respectively 24 hours later (P<0.05): 8.1%+/-2.3%, 26.9%+/-4.2%, 35.6%+/-3.8%, 56.5%+/-6.1%, and 69.8%+/-5.3% 48 h later (P<0.05); and 10.5%+/-1.3%, 28.4%+/-3.2%, 50.5%+/-5.8%, 70.5%+/-6.9%, and 78.6%+/-4.5% 72 h later (P<0.05). "( [Experimental study on the effect of trichostatin A on differentiation of human lung carcinoma cell].
Meng, M; Wang, CT, 2007
)
2.06
"Trichostatin A treatment did not modify MBD1 binding to the ABCB1 promoter and similarly increased PCAF binding in both H69 cell lines."( The histone deacetylase inhibitor trichostatin A downregulates human MDR1 (ABCB1) gene expression by a transcription-dependent mechanism in a drug-resistant small cell lung carcinoma cell line model.
Breuzard, G; Dufer, J; El-Khoury, V; Fourré, N, 2007
)
1.34
"Trichostatin A treatment results in dramatic reactivation of gene expression that is preceded by histone acetylation and chromatin decondensation."( Molecular mechanism for silencing virally transduced genes involves histone deacetylation and chromatin condensation.
Chen, WY; Townes, TM, 2000
)
1.03
"Trichostatin A treatment arrests cells at the G(2)-M phase of the cell cycle, which is consistent with the hypothesis that the proper formation of the chromatin after DNA replication may be important in signaling the progression through the cell cycle."( Proliferating cell nuclear antigen associates with histone deacetylase activity, integrating DNA replication and chromatin modification.
Milutinovic, S; Szyf, M; Zhuang, Q, 2002
)
1.04
"Pretreatment with trichostatin A, a pan-histone deacetylase inhibitor that renders chromatin decondensation, significantly decreased the number of mutations in UVB-irradiated keratinocytes."( Exome sequencing identifies novel mutation signatures of UV radiation and trichostatin A in primary human keratinocytes.
Ha, W; Liu, L; Queen, D; Shen, Y; Zeng, W, 2020
)
1.11
"Pre-treatment of trichostatin A significantly hampered glomerulosclerosis and tubulointerstitial fibrosis, as did the pre-treatment with valproic acid."( Comparison of trichostatin A and valproic acid treatment regimens in a mouse model of kidney fibrosis.
Geers, C; Mannaerts, I; Pauwels, M; Van Beneden, K; Van den Branden, C; van Grunsven, LA; Wissing, KM, 2013
)
1.08
"Treatment with Trichostatin A, relaxing chromatin, recovers both transcription initiation and UV-survival."( Histone methyltransferase DOT1L drives recovery of gene expression after a genotoxic attack.
Coin, F; Eberova, J; Egly, JM; Giglia-Mari, G; Mari, PO; Nardo, T; Oksenych, V; Stefanini, M; Zhovmer, A; Ziani, S, 2013
)
0.73
"Treatment with trichostatin A, a histone deacetylase inhibitor, predominantly up-regulated NDRG2 expression in the NDRG2 low-expressing cell lines (PANC-1, PCI-35, PK-45P, and AsPC-1)."( Suppressed expression of NDRG2 correlates with poor prognosis in pancreatic cancer.
Abe, K; Egawa, S; Fukushige, S; Horii, A; Kaneko, N; Karasawa, H; Miura, K; Mizuguchi, Y; Morishita, K; Motoi, F; Nagase, H; Saiki, Y; Sasaki, I; Sase, T; Shibata, C; Sunamura, M; Unno, M; Yamamura, A, 2013
)
0.73
"Pretreatment with trichostatin A decreased amylase levels by 70 % and protected against tissue injury in the pancreas. "( Histone deacetylase regulates trypsin activation, inflammation, and tissue damage in acute pancreatitis in mice.
Hartman, H; Regnér, S; Thorlacius, H; Wetterholm, E, 2015
)
0.75
"Treatment with trichostatin A (TSA) led to defective callus formation on callus-inducing medium (CIM)."( Histone deacetylation-mediated cellular dedifferentiation in Arabidopsis.
Jung, SJ; Lee, K; Park, OS; Seo, PJ, 2016
)
0.77
"Treatment with Trichostatin A (TSA), a broad-spectrum HDAC inhibitor, restored their physical association, and attenuated Ang-II-induced MMP9 expression, IL-18 induction, and extracellular matrix (collagen I, collagen III and fibronectin) production."( Histone deacetyltransferase inhibitors Trichostatin A and Mocetinostat differentially regulate MMP9, IL-18 and RECK expression, and attenuate Angiotensin II-induced cardiac fibroblast migration and proliferation.
Chandrasekar, B; Higashi, Y; Krenz, M; McDonald, KS; Noda, M; Somanna, NK; Valente, AJ, 2016
)
1.04
"Treatment with trichostatin A led to enhanced acetylation of histone H3-K9 with concurrent induction of E-cadherin mRNA in 3 E-cadherin low/negative cell lines that are not DNA methylated."( Histone H3 (lys-9) deacetylation is associated with transcriptional silencing of E-cadherin in colorectal cancer cell lines.
Eu, KW; Hong, Y; Ismail, TM; Liu, Y; Wong, Y; Zhao, Y, 2008
)
0.69
"Co-treatment with trichostatin A maintained near-normal levels of acetylation of histone core proteins in cochlear hair cells and attenuated gentamicin-induced cell death."( Aminoglycoside-induced histone deacetylation and hair cell death in the mouse cochlea.
Chen, FQ; Schacht, J; Sha, SH, 2009
)
0.68
"Treatment with trichostatin A, a classical HDAC inhibitor, also decreased pathogenesis."( Inhibition of histone deacetylase causes reduction of appressorium formation in the rice blast fungus Magnaporthe oryzae.
Arie, T; Izawa, M; Kamakura, T; Kimura, M; Takekawa, O; Teraoka, T; Yoshida, M, 2009
)
0.69
"Treatment with trichostatin A at 50 ng/mL decreased the collagen level in cells from neurogenic bladders to almost normal levels (2.1 microg/mL)."( The effect of epigenetic therapy on congenital neurogenic bladders--a pilot study.
Atala, A; Hodges, SJ; Mishra, N; Yoo, JJ, 2010
)
0.7
"Treatment with trichostatin A or apicidine suppressed the proliferation in all cell lines examined, in association with increased expression of p21 and down-regulation of cyclin D1 and cyclin A expression."( Immunohistochemical detection of histone deacetylases in endometrial carcinoma: involvement of histone deacetylase 2 in the proliferation of endometrial carcinoma cells.
Fakhry, H; Kashima, H; Ke, H; Konishi, I; Miyamoto, T; Shiozawa, T; Suzuki, A, 2010
)
0.7
"Treatment with trichostatin A, which inhibits histone deacetylases, resulted in increased histone H4 acetylation accompanied by the decondensation of interphase chromatin and a decrease in both global H3K9 dimethylation and DNA methylation during mitosis in maize root tip cells. "( Trichostatin A and 5-azacytidine both cause an increase in global histone H4 acetylation and a decrease in global DNA and H3K9 methylation during mitosis in maize.
Huang, J; Li, J; Li, L; Ma, L; Wen, R; Yang, F; Zhang, L; Zhou, D, 2010
)
2.16
"Treatment with trichostatin A and 5-azacytidine treatment caused a decrease in the mitotic index, suggesting that H4 deacetylation and DNA and H3K9 methylation may contain the necessary information for triggering mitosis in maize root tips."( Trichostatin A and 5-azacytidine both cause an increase in global histone H4 acetylation and a decrease in global DNA and H3K9 methylation during mitosis in maize.
Huang, J; Li, J; Li, L; Ma, L; Wen, R; Yang, F; Zhang, L; Zhou, D, 2010
)
2.14
"Treatment with Trichostatin A alone had no significant effect on the expression of PCDH10 but enhanced the effect of 5'-azacytidin."( Epigenetic inactivation of PCDH10 in human prostate cancer cell lines.
Cai, Z; Gui, Y; Li, W; Li, X; Li, Z; Tang, A; Wang, Y; Xie, J; Ye, J, 2011
)
0.71
"Treatment with trichostatin A, a histone deacetylase inhibitor, blocks chromatin structural changes but not nuclear tyrosine phosphorylation by c-Abl."( Nuclear c-Abl-mediated tyrosine phosphorylation induces chromatin structural changes through histone modifications that include H4K16 hypoacetylation.
Aoyama, K; Fukumoto, Y; Horiike, Y; Ishibashi, K; Kubota, S; Morinaga, T; Nakayama, Y; Takahashi, A; Yamaguchi, N; Yuki, R, 2011
)
0.71
"Treatment with trichostatin A, but not other histone deacetylase inhibitors, partially restored reelin transcription and promoted the accumulation of mutant ATXN7 into nuclear inclusions."( Reelin is a target of polyglutamine expanded ataxin-7 in human spinocerebellar ataxia type 7 (SCA7) astrocytes.
Bekiranov, S; Dent, SY; Grant, PA; McCullough, SD; Roeder, RG; Xu, X, 2012
)
0.72
"Treatment with trichostatin A, a histone deacetylase inhibitor, resulted in hTERT reactivation only in very early differentiating HT cells."( Control mechanisms in the regulation of telomerase reverse transcriptase expression in differentiating human teratocarcinoma cells.
Andrews, LG; Hansen, NJ; Key, JS; Lopatina, NG; Pita, MA; Poole, JC; Saldanha, SN; Tollefsbol, TO, 2003
)
0.66
"Treatment with trichostatin A, which is an inhibitor of histone deacetylase, or PML over-expression relieved Daxx-mediated transcriptional repression of p53."( Identification of Daxx interacting with p73, one of the p53 family, and its regulation of p53 activity by competitive interaction with PML.
Kim, EJ; Park, JS; Um, SJ, 2003
)
0.66
"Treatment with trichostatin A and calphostin C led to a 50% to 90% decrease of trichostatin A- mediated upregulation of nuclear factor kappaB and p21 activation."( Induction of apoptosis of lung and esophageal cancer cells treated with the combination of histone deacetylase inhibitor (trichostatin A) and protein kinase C inhibitor (calphostin C).
Cole, GW; Maxhimer, JB; Nguyen, DM; Reddy, RM; Schrump, DS; Zuo, J, 2005
)
0.88
"Cotreatment with trichostatin A and cycloheximide restored TS mRNA expression, suggesting that TS mRNA is repressed through new protein synthesis."( Histone deacetylase inhibitor enhances 5-fluorouracil cytotoxicity by down-regulating thymidylate synthase in human cancer cells.
Bang, YJ; Jong, HS; Jung, Y; Kim, JH; Kim, TY; Lee, JH; Park, JH, 2006
)
0.66
"Treatment with trichostatin A (TSA), an inhibitor of histone deacetylases, induced histone hyperacetylation of meiotic chromosomes from which endogenous BRD4, however, remained dissociated."( Histone acetylation and subcellular localization of chromosomal protein BRD4 during mouse oocyte meiosis and mitosis.
Arase, T; Furuya, M; Kajitani, T; Maruyama, T; Masuda, H; Nagashima, T; Ono, M; Ozato, K; Uchida, H; Yoshimura, Y, 2007
)
0.68
"Treatment with trichostatin A, a potent inhibitor of the transcriptional co-repressor HDAC, partially reversed the inhibitory effect of BCL3."( BCL3 acts as a negative regulator of transcription from the human T-cell leukemia virus type 1 long terminal repeat through interactions with TORC3.
Ego, T; Hishiki, T; Ohshima, T; Shimotohno, K, 2007
)
0.68
"Treatment with trichostatin A, a specific inhibitor of histone deacetylase, reduces the expression of the active maternal H19 allele and this can be correlated with regional changes in acetylation within the upstream regulatory domain."( Relationship between DNA methylation, histone H4 acetylation and gene expression in the mouse imprinted Igf2-H19 domain.
Ferguson-Smith, A; Grandjean, V; O'Neill, L; Sado, T; Turner, B, 2001
)
0.65

Toxicity

ExcerptReferenceRelevance
" This combination was not toxic to primary normal cells."( Rapid and profound potentiation of Apo2L/TRAIL-mediated cytotoxicity and apoptosis in thoracic cancer cells by the histone deacetylase inhibitor Trichostatin A: the essential role of the mitochondria-mediated caspase activation cascade.
Baras, A; Chua, A; Maxhimer, JB; Nguyen, DM; Reddy, RM; Schrump, DS; Shamimi-Noori, SM; Yeow, WS; Ziauddin, MF, 2007
)
0.54
" Coexposure of LBH589 and bortezomib at minimally toxic doses of either drug alone resulted in a striking induction of apoptosis in established U251, U87, and D37 GBM cell lines, as well as in GBM8, GBM10, GBM12, GBM14, and GBM56 short-term cultured cell lines."( Mitochondrial Bax translocation partially mediates synergistic cytotoxicity between histone deacetylase inhibitors and proteasome inhibitors in glioma cells.
Adjei, AA; Atadja, P; Friday, BB; Sarkaria, J; Wigle, D; Yang, L; Yu, C, 2008
)
0.35
"Radiation-induced gastrointestinal injury (RIGI) is a serious side effect of abdominal and pelvic radiotherapy, which often limits the treatment of gastrointestinal and gynaecological cancers."( Mitigative and anti-inflammatory effects of Trichostatin A against radiation-induced gastrointestinal toxicity and gut microbiota alteration in mice.
Agrawala, PK; Dahiya, A; Dutta, A, 2023
)
1.17

Compound-Compound Interactions

Valproic acid, trichostatin and their combination with hemin (all three FDA-approved drugs) preferentially increase gamma-globin chain synthesis and may be helpful for the treatment of hemoglobinopathies. We explored the anti-cancer efficiency of HPV targeted ZFNs combined with a platinum-based antineoplastic drug Cisplatin (DDP) and an HDAC inhibitor Trichostati A (TSA)

ExcerptReferenceRelevance
" As203 alone or in combination with ATRA induced neither differentiation nor apoptosis."( Histone deacetylase inhibitor but not arsenic trioxide differentiates acute promyelocytic leukaemia cells with t(11;17) in combination with all-trans retinoic acid.
Hoshi, S; Kitamura, K; Kiyoi, H; Koike, M; Naoe, T; Saito, H, 2000
)
0.31
" In this study we tested the effect of valproic acid and trichostatin, alone or in combination with hemin, on gamma chain synthesis in human erythroid liquid cultures."( Valproic acid, trichostatin and their combination with hemin preferentially enhance gamma-globin gene expression in human erythroid liquid cultures.
Akel, S; Kollia, P; Loukopoulos, D; Marianna, P; Papassotiriou, Y; Stamoulakatou, A, 2001
)
0.66
"Valproic acid, trichostatin and their combination with hemin (all three FDA-approved drugs) preferentially increase gamma-globin chain synthesis and may be helpful for the treatment of hemoglobinopathies."( Valproic acid, trichostatin and their combination with hemin preferentially enhance gamma-globin gene expression in human erythroid liquid cultures.
Akel, S; Kollia, P; Loukopoulos, D; Marianna, P; Papassotiriou, Y; Stamoulakatou, A, 2001
)
1.02
" HDAC inhibitors combined with paclitaxel may enhance the inhibitory effect of drugs on lung cancer cells."( [Synergistic cytotoxicity effect of histone deacetylase inhibitor combined with paclitaxel on lung cancer cell lines and its mechanism].
Liu, CT; Liu, Y; Yu, XD; Zhang, D, 2009
)
0.35
"When combined with TSA, the 50% inhibition concentration (IC50) of paclitaxel decreased from (48."( [Synergistic cytotoxicity effect of histone deacetylase inhibitor combined with paclitaxel on lung cancer cell lines and its mechanism].
Liu, CT; Liu, Y; Yu, XD; Zhang, D, 2009
)
0.35
"TSA combined with paclitaxel has a synergistic cytotoxicity effect on lung cancer cell lines H322 and H1299 when the cells were treated with TSA followed by paclitaxel."( [Synergistic cytotoxicity effect of histone deacetylase inhibitor combined with paclitaxel on lung cancer cell lines and its mechanism].
Liu, CT; Liu, Y; Yu, XD; Zhang, D, 2009
)
0.35
"To explore the effect of trichostatin A (TSA) alone and combination with imatinib on the proliferation and apoptosis of K562R cells."( [Effect of trichostatin alone and combination with imatinb on the proliferation and apoptosis of the K562R cells].
Chen, F; Chen, S; He, Q; Liu, Y; Zeng, H; Zhao, X, 2011
)
1.06
" Combined with imatinib, the effect of proliferation inhibition was better."( [Effect of trichostatin alone and combination with imatinb on the proliferation and apoptosis of the K562R cells].
Chen, F; Chen, S; He, Q; Liu, Y; Zeng, H; Zhao, X, 2011
)
0.76
"TSA combined with imatinib can inhibit the proliferation of K562R cells and induce its apopotosis."( [Effect of trichostatin alone and combination with imatinb on the proliferation and apoptosis of the K562R cells].
Chen, F; Chen, S; He, Q; Liu, Y; Zeng, H; Zhao, X, 2011
)
0.76
" Our study highlights the molecular targetability of HDACs 1, 7, and 8, confirm their PDAC-CSCs maintaining role, and demonstrate that compared to SAHA, TSA modulates the epigenetically- mediated oncogenic activity of PDAC-CSCs, and potentiate Gemcitabine therapeutic activity, making a case for further exploration of TSA activity alone or in combination with Gemcitabine in PDAC therapy."( Depletion of HDAC1, 7 and 8 by Histone Deacetylase Inhibition Confers Elimination of Pancreatic Cancer Stem Cells in Combination with Gemcitabine.
Cai, MH; Sun, Z; Tu, YX; Wang, BK; Xu, XG; Yan, SL; Ying, Y, 2018
)
0.48
" The present study was designed to investigate the effect of zebularine in comparison to and in combination with trichostatin A on p21Cip1/Waf1/Sdi1, p27Kip1, p57Kip2, DNMT1, DNMT3a and DNMT3b, Class I HDACs (HDACs 1, 2, 3) and Class II HDACs (HDACs 4, 5, 6) gene expression, cell growth inhibition and apoptosis induction in colon cancer LS 174T cell line."( Effect of Zebularine in Comparison to and in Combination with Trichostatin A on CIP/KIP Family (p21Cip1/Waf1/Sdi1, p27Kip1, and p57Kip2), DNMTs (DNMT1, DNMT3a, and DNMT3b), Class I HDACs (HDACs 1, 2, 3) and Class II HDACs (HDACs 4, 5, 6) Gene Expression,
Kavoosi, F; Sanaei, M, 2020
)
1.01
" We here explored the anti-cancer efficiency of HPV targeted ZFNs combined with a platinum-based antineoplastic drug Cisplatin (DDP) and an HDAC inhibitor Trichostatin A (TSA)."( The Antitumor Efficiency of Zinc Finger Nuclease Combined with Cisplatin and Trichostatin A in Cervical Cancer Cells.
Ding, W; Gao, C; Li, X; Ren, C; Shen, H; Wang, H; Wang, L; Wu, P; Xiong, J; Zhu, D, 2020
)
0.98
"Our results demonstrated that ZFNs combined with DDP or TSA functioned effectively in cervical cancer cells, and it provided novel ideas for the prevention and treatment of HPV-related cervical malignancies."( The Antitumor Efficiency of Zinc Finger Nuclease Combined with Cisplatin and Trichostatin A in Cervical Cancer Cells.
Ding, W; Gao, C; Li, X; Ren, C; Shen, H; Wang, H; Wang, L; Wu, P; Xiong, J; Zhu, D, 2020
)
0.79

Bioavailability

ExcerptReferenceRelevance
" In this study we have synthesized and evaluated compounds that combine the bioavailability of short-chain fatty acids, like butyric acid, with the bidentate binding ability of TSA."( Simple inhibitors of histone deacetylase activity that combine features of short-chain fatty acid and hydroxamic acid inhibitors.
Abuaita, B; Cuthpert, SC; Fage, C; Furr, EB; Hedrick, J; Meyers, J; Murphy, K; Saxe, A; Snare, D; Tischler, JL; Zand, AR, 2008
)
0.35
"New orally bioavailable 5-(thiophen-2-yl)-substituted 2-aminobenzamide-series histone deacetylase inhibitors were synthesized."( Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
Baba, K; Hirata, M; Hirata, Y; Kawaratani, Y; Nagaoka, Y; Ohmomo, Y; Shibano, M; Taniguchi, M; Uesato, S; Yasuda, M, 2012
)
0.38
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Xc1-mediated repression can be only partially alleviated by an increase in transcription factor dosage. Inhibition of deacetylase activity by trichostatin A treatment has no effect on XPc1 repression.

ExcerptRelevanceReference
" Dose-response curves and kinetic analysis show a close correlation between the level of histone acetylation and HIV-1 gene expression."( Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation.
Emiliani, S; Ott, M; Van Lint, C; Verdin, E, 1996
)
0.29
" Dose-response and kinetic analysis suggest a close correlation between the level of histone acetylation and the induction of the WAF1/Cip1 expressions."( Histone deacetylase inhibitor activates the WAF1/Cip1 gene promoter through the Sp1 sites.
Minamikawa, S; Mizuno, T; Nakano, K; Nomura, H; Orita, T; Sakai, T; Sowa, Y, 1997
)
0.3
" We find that XPc1-mediated repression can be only partially alleviated by an increase in transcription factor dosage and that inhibition of deacetylase activity by trichostatin A treatment has no effect on XPc1 repression, suggesting that histone deacetylation does not form the basis for Pc-G-mediated repression in our assay."( Transcriptional repression by XPc1, a new Polycomb homolog in Xenopus laevis embryos, is independent of histone deacetylase.
Damjanovski, S; Meric, F; Strouboulis, J; Vermaak, D; Wolffe, AP, 1999
)
0.5
" TSA also prevented, in a dose-response relationship, the sprouting of capillaries from rat aortic rings."( Histone deacetylases inhibitors as anti-angiogenic agents altering vascular endothelial growth factor signaling.
Blacher, S; Bonjean, K; Castronovo, V; Clausse, N; Colige, A; Deroanne, CF; Devy, L; Foidart, JM; Nusgens, BV; Servotte, S; Verdin, E, 2002
)
0.31
" Four compounds having an MTD > or = 100 mg/kg were selected for dose-response studies in the HCT116 xenograft model."( N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
Atadja, P; Bair, KW; Bontempo, J; Cesarz, D; Chandramouli, N; Chen, R; Cheung, M; Cornell-Kennon, S; Dean, K; Diamantidis, G; France, D; Green, MA; Howell, KL; Kashi, R; Kwon, P; Lassota, P; Martin, MS; Mou, Y; Perez, LB; Remiszewski, SW; Sambucetti, LC; Sharma, S; Smith, T; Sorensen, E; Taplin, F; Trogani, N; Versace, R; Walker, H; Weltchek-Engler, S; Wood, A; Wu, A, 2003
)
0.32
" The concordance is apparent both by en masse correlation of fold-changes and by detailed similarity of dose-response profiles of individual genes."( Association of valproate-induced teratogenesis with histone deacetylase inhibition in vivo.
Berman, MG; Gentleman, RC; Green, JB; Gurvich, N; Klein, PS; Wittner, BS, 2005
)
0.33
" Dose-response correlations and the duration of response to aza-deoxycytidine (ADC) and trichostatin A (TSA) were characterized."( Epigenetic-mediated upregulation of progesterone receptor B gene in endometrial cancer cell lines.
Dowdy, SC; Eberhardt, NL; Gonzalez Bosquet, J; Jiang, SW; Podratz, KC; Xiong, Y; Zhao, Y, 2005
)
0.55
" Dose-response curves showed that a concentration of 333 nM TSA was optimal in inducing AChE expression."( Histone acetylase inhibitor trichostatin A induces acetylcholinesterase expression and protects against organophosphate exposure.
Compton, JR; Curtin, BF; Doctor, BP; Gordon, RK; Nambiar, MP; Tetz, LM, 2005
)
0.62
"Varying the concentration of selected factors alters the induction properties of steroid receptors by changing the position of the dose-response curve (or the value for half-maximal induction=EC(50)) and the amount of partial agonist activity of antisteroids."( Effects of acetylation, polymerase phosphorylation, and DNA unwinding in glucocorticoid receptor transactivation.
Chow, C; Kim, Y; Pommier, YG; Simons, SS; Sun, Y, 2006
)
0.33
" Here we show that dosage sensitivity is associated with the differential histone H3/H4 acetylation states of Nkx3."( Haploinsufficient prostate tumor suppression by Nkx3.1: a role for chromatin accessibility in dosage-sensitive gene regulation.
Abdulkadir, SA; Crooke, PS; Mogal, AP; van der Meer, R, 2007
)
0.34
" Synergy is dependent on viral replication; however, it is not dependent on the dosing sequence of TSA and G47Delta, viral genetic alterations, infectivity, or replication kinetics of G47Delta."( Trichostatin A and oncolytic HSV combination therapy shows enhanced antitumoral and antiangiogenic effects.
Castelo-Branco, P; Liu, TC; Martuza, RL; Rabkin, SD, 2008
)
1.79
" Numerous transcription factors are known to modulate three parameters of gene induction: the total activity (Vmax) and position of the dose-response curve with glucocorticoids (EC50) and the percent partial agonist activity with antiglucocorticoids."( Modulation of transcription parameters in glucocorticoid receptor-mediated repression.
He, Y; Kagan, BL; Simons, SS; Sun, Y; Tao, YG, 2008
)
0.35
" The dose-response curve of DHT-stimulated C4-2 colony formation was shifted by shHDAC6 such that approximately 10-fold higher concentration of DHT is required, indicating a requirement for HDAC6 in AR hypersensitivity."( HDAC6 regulates androgen receptor hypersensitivity and nuclear localization via modulating Hsp90 acetylation in castration-resistant prostate cancer.
Ai, J; Dar, JA; Liu, J; Liu, L; Nelson, JB; Wang, Y; Wang, Z, 2009
)
0.35
" Daily histone deacetylase (HDAC) inhibitor infusions in the shell of the nucleus accumbens (NAc) caused an upward shift in the dose-response curve under fixed-ratio schedule and increased the break point under progressive-ratio schedule, indicating enhanced motivation for self-administered drug."( Chronic cocaine-induced H3 acetylation and transcriptional activation of CaMKIIalpha in the nucleus accumbens is critical for motivation for drug reinforcement.
Hu, Z; Hui, B; Lv, Z; Ma, L; Sheng, J; Sun, J; Wang, L, 2010
)
0.36
"During initial development, both X chromosomes are active in females, and one of them must be silenced at the appropriate time in order to dosage compensate their gene expression levels to male counterparts."( HDAC inhibition decreases XIST expression on female IVP bovine blastocysts.
Cruz, MH; Garcia, JM; Lopes, FL; Mazeti, B; Oliveira, CS; Oliveira, LZ; Saraiva, NZ, 2013
)
0.39
" Our results showed that TSA caused an elevated level of cellular acetylation and conformational/structural changes of proteins in the cells, and a higher dosage of TSA caused a higher percent of α-helix structure accompanied by an increment of acetylation level in both histones and cytoskeleton proteins."( Assessment of the effect of trichostatin A on HeLa cells through FT-IR spectroscopy.
Huang, Q; Li, J; Yan, J; Zhang, F; Zhang, X, 2015
)
0.71
" To determine the role of gene overexpression on chromosome instability (CIN), we performed genome-wide screens in the budding yeast for yeast genes that cause CIN when overexpressed, a phenotype we refer to as dosage CIN (dCIN), and identified 245 dCIN genes."( Overexpression screens identify conserved dosage chromosome instability genes in yeast and human cancer.
Andrews, B; Ang, JS; Boerkoel, CF; Duffy, S; Fam, HK; Hieter, P; Kim, JH; Larionov, V; Shah, SP; Singh, T; Styles, EB; Wang, YK, 2016
)
0.43
"SAHA and TSA could inhibit total HDAC activity and placental HDAC1/2/3 expression both in Bewo and JAR, but displayed a transient induction of HDAC mRNA or protein level after being treated at low dosage or prolonged exposure to drugs."( The effect of histone deacetylase inhibition on the expression of P-glycoprotein in human placental trophoblast cell lines.
Duan, H; Hua, Y; Li, Q; Li, Y; Qiu, D; Wang, C; Wang, T; Zhang, Y; Zhou, K, 2017
)
0.46
" The sensitivity of the high-throughput cell mechanical measurements to the cytoskeletal modifications we present in this study opens up new possibilities for label-free dose-response assays of cytoskeletal modifications."( High-throughput cell mechanical phenotyping for label-free titration assays of cytoskeletal modifications.
Golfier, S; Guck, J; Herbig, M; Mietke, A; Otto, O; Rosendahl, P, 2017
)
0.46
" We applied dosing schedules."( Trichostatin A, a histone deacetylase inhibitor, alleviates the emotional abnormality induced by maladaptation to stress in mice.
Kimijima, H; Kurokawa, K; Miyagawa, K; Mochida-Saito, A; Takahashi, K; Takeda, H; Tsuji, M, 2022
)
2.16
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
bacterial metaboliteAny prokaryotic metabolite produced during a metabolic reaction in bacteria.
geroprotectorAny compound that supports healthy aging, slows the biological aging process, or extends lifespan.
EC 3.5.1.98 (histone deacetylase) inhibitorAn EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
trichostatin
hydroxamic acidA compound, RkE(=O)lNHOH, derived from an oxoacid RkE(=O)l(OH) (l =/= 0) by replacing -OH with -NHOH, and derivatives thereof. Specific examples of hydroxamic acids are preferably named as N-hydroxy amides.
antibiotic antifungal agentHeteroorganic entities that are microbial metabolites (or compounds derived from them) which have significant antifungal properties.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (71)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID485281
ATAD5 protein, partialHomo sapiens (human)Potency11.53660.004110.890331.5287AID624247; AID624252; AID624253; AID686934; AID720565
PPM1D proteinHomo sapiens (human)Potency2.08210.00529.466132.9993AID1347411
Microtubule-associated protein tauHomo sapiens (human)Potency35.48130.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency37.68580.531815.435837.6858AID504845
glucocerebrosidaseHomo sapiens (human)Potency17.78280.01268.156944.6684AID2101
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.84890.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency6.92410.016525.307841.3999AID602332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
survival motor neuron protein isoform dHomo sapiens (human)Potency1.26730.125912.234435.4813AID1458; AID1740
Interferon betaHomo sapiens (human)Potency2.08210.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HDLP (HISTONE DEACETYLASE-LIKE PROTEIN)Aquifex aeolicusIC50 (µMol)0.40000.40000.40000.4000AID977608
Chain B, HDLP (HISTONE DEACETYLASE-LIKE PROTEIN)Aquifex aeolicusIC50 (µMol)0.40000.40000.40000.4000AID977608
Chain A, Histone deacetylase 7aHomo sapiens (human)IC50 (µMol)0.30000.30000.30000.3000AID977608
Chain A, Histone deacetylase 7aHomo sapiens (human)IC50 (µMol)0.30000.30000.30000.3000AID977608
Histone deacetylase 8Schistosoma mansoniIC50 (µMol)3.62000.30341.33503.6200AID1446915
Histone deacetylase Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Lysine-specific demethylase 4EHomo sapiens (human)IC50 (µMol)28.40000.20001.95696.3096AID1885254
Histone deacetylase 1Mus musculus (house mouse)IC50 (µMol)0.00430.00140.72308.1000AID273173; AID316880; AID90519; AID90673; AID90675; AID90680; AID90681
Histone deacetylase 1Mus musculus (house mouse)Ki0.00110.00110.03430.0676AID90677
Histone deacetylase 3Homo sapiens (human)IC50 (µMol)0.33880.00040.619610.0000AID1127324; AID1173704; AID1246509; AID1273502; AID1280315; AID1294973; AID1322059; AID1324228; AID1354393; AID1363779; AID1384761; AID1394890; AID1459968; AID1532631; AID1586079; AID1605940; AID1622918; AID1647301; AID1690108; AID1758520; AID1765326; AID1781513; AID1802398; AID1802451; AID1863435; AID1901146; AID242687; AID286454; AID316875; AID316888; AID331898; AID331899; AID366642; AID382342; AID408882; AID417646; AID420326; AID447991; AID447992; AID447994; AID456795; AID463865; AID465151; AID478330; AID488275; AID525002; AID539709; AID541646; AID568152; AID608776; AID723479; AID723726; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 3Homo sapiens (human)Ki0.08440.00020.42378.1900AID1236444; AID1479815; AID331899; AID447579; AID487226; AID496803
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)IC50 (µMol)7.69000.69004.19007.6900AID568153
Histone deacetylase 3Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Plasma kallikreinHomo sapiens (human)IC50 (µMol)0.03400.00312.024110.0000AID269912
Integrin beta-3Homo sapiens (human)IC50 (µMol)0.02630.00010.632310.0000AID242561
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)0.02000.00011.774010.0000AID1354391; AID1390224
Integrin alpha-IIbHomo sapiens (human)IC50 (µMol)0.02630.00010.730910.0000AID242561
Coagulation factor VIIHomo sapiens (human)IC50 (µMol)0.03400.00020.83363.3000AID269912
Leukotriene A-4 hydrolaseHomo sapiens (human)IC50 (µMol)10.00000.00051.28547.6500AID1441630; AID1441631
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.00500.00002.015110.0000AID708216
Vitamin D3 receptorHomo sapiens (human)IC50 (µMol)0.08700.00000.43746.4300AID1915533
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.02800.00002.800510.0000AID1390224
Tissue factorHomo sapiens (human)IC50 (µMol)0.03200.00010.734410.0000AID269912; AID360092; AID360093; AID360094; AID360095; AID385446; AID385447
Adenosine receptor A1Bos taurus (cattle)IC50 (µMol)0.19000.00001.09106.7400AID313185
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.00500.00002.398310.0000AID708216
Delta-type opioid receptorHomo sapiens (human)IC50 (µMol)0.10000.00020.75218.0140AID80353
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.10000.00402.15557.2000AID80353
Histone deacetylase 4Homo sapiens (human)IC50 (µMol)0.85520.00061.052610.0000AID1127325; AID1173704; AID1182187; AID1246514; AID1273502; AID1530556; AID1578487; AID1622920; AID1622967; AID1781513; AID1802398; AID1802451; AID1847776; AID1901151; AID240718; AID242687; AID269912; AID286454; AID302798; AID308644; AID309968; AID313186; AID316875; AID316888; AID331616; AID331898; AID382342; AID417647; AID420326; AID447991; AID447992; AID456795; AID461092; AID463865; AID478330; AID525000; AID539709; AID541648; AID568153; AID608776; AID628435; AID695594; AID723464; AID723479; AID723726; AID764213; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 4Homo sapiens (human)Ki3.65020.00021.62559.1242AID1236446; AID1622973; AID447579; AID496804; AID760387
Histone deacetylase 2Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)0.41910.00010.55439.9000AID1127323; AID1173704; AID1173705; AID1182186; AID1246507; AID1254047; AID1273502; AID1276711; AID1280314; AID1294953; AID1322059; AID1322060; AID1322066; AID1324226; AID1354391; AID1363777; AID1384206; AID1384759; AID1390223; AID1394889; AID1401557; AID1432957; AID1459953; AID1518781; AID1525777; AID1530555; AID1532629; AID1557981; AID1578485; AID1586077; AID1589336; AID1591715; AID1605938; AID1622916; AID1622966; AID1647311; AID1651332; AID1652187; AID1659230; AID1690107; AID1709382; AID1758519; AID1764791; AID1765324; AID1781513; AID1802398; AID1802451; AID1833063; AID1863433; AID1882456; AID1901147; AID240717; AID242687; AID254791; AID269911; AID273990; AID286454; AID302797; AID308643; AID309967; AID313185; AID316875; AID316888; AID331615; AID331898; AID366640; AID382342; AID408880; AID417644; AID420325; AID420326; AID447991; AID447992; AID447993; AID456795; AID461091; AID463865; AID465149; AID478330; AID488273; AID488358; AID525003; AID538408; AID539709; AID541644; AID568150; AID608776; AID611683; AID621737; AID628437; AID650229; AID654541; AID659292; AID683274; AID695592; AID708216; AID723466; AID723479; AID723726; AID756022; AID764214; AID769934; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529; AID90661; AID90662; AID90666; AID90668
Histone deacetylase 1Homo sapiens (human)Ki0.07230.00000.49888.1900AID1236442; AID1479814; AID1622972; AID447579; AID487224; AID496801; AID760390
Splicing factor 3B subunit 3Homo sapiens (human)IC50 (µMol)0.59440.01090.93893.4810AID506784; AID507021
Histone deacetylase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.34513.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Adenosine receptor A1Sus scrofa (pig)IC50 (µMol)0.20000.20000.20000.2000AID313186
Histone deacetylase Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Histone deacetylase 4Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Polyamine deacetylase HDAC10Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Histone deacetylase 3Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188IC50 (µMol)1.20001.00001.10001.2000AID420318
Histone deacetylase-like amidohydrolaseAlcaligenaceae bacterium FB188Ki0.70000.70003.05009.2000AID420317
Histone deacetylase 7Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
NAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)Ki226.00002.00002.00002.0000AID1423498; AID1423503
Histone deacetylase 8Mus musculus (house mouse)IC50 (µMol)0.02070.00140.02070.0400AID90519; AID90840
Histone deacetylase 7Homo sapiens (human)IC50 (µMol)0.50520.00071.02609.9000AID1127328; AID1173704; AID1246516; AID1273502; AID1578489; AID1622922; AID1781513; AID1802398; AID1802451; AID242687; AID286454; AID316875; AID316888; AID331898; AID382342; AID417650; AID420326; AID447991; AID447992; AID456795; AID463865; AID478330; AID524997; AID539709; AID541650; AID608776; AID628432; AID723479; AID723726; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 7Homo sapiens (human)Ki0.29800.00022.00059.5000AID1236448; AID447579; AID496807
Histone deacetylase 11Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Histone deacetylase 2Homo sapiens (human)IC50 (µMol)0.64010.00010.72219.9700AID1173704; AID1173706; AID1246508; AID1273502; AID1276706; AID1294963; AID1322059; AID1324227; AID1354392; AID1363778; AID1384760; AID1401558; AID1459954; AID1578486; AID1586078; AID1605939; AID1622917; AID1630587; AID1647300; AID1651333; AID1765325; AID1781513; AID1802398; AID1802451; AID1833064; AID1863434; AID242687; AID254792; AID286454; AID316875; AID316888; AID331898; AID366641; AID367237; AID382342; AID408881; AID417645; AID420326; AID447991; AID447992; AID456795; AID463865; AID465150; AID478330; AID488274; AID525001; AID539709; AID541645; AID568151; AID608776; AID611684; AID628436; AID650228; AID659293; AID723465; AID723479; AID723726; AID756023; AID769935; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 2Homo sapiens (human)Ki0.08510.00000.47098.1900AID1236443; AID1479811; AID447579; AID487225; AID496802; AID760389
HD2 type histone deacetylase HDA106 Zea maysIC50 (µMol)0.00600.00300.17372.0000AID241474; AID273166; AID90197; AID90359; AID90682; AID90687; AID90688; AID90690; AID90691; AID90695; AID90696
HD2 type histone deacetylase HDA106 Zea maysKi0.00440.00440.06810.1318AID90199; AID90693
Polyamine deacetylase HDAC10Homo sapiens (human)IC50 (µMol)0.32660.00050.72459.9000AID1127331; AID1173704; AID1246512; AID1273502; AID1294971; AID1384758; AID1401561; AID1459974; AID1578491; AID1586085; AID1605947; AID1622925; AID1781513; AID1802398; AID1802451; AID242687; AID286454; AID316875; AID316888; AID331898; AID366645; AID382342; AID408884; AID417653; AID420326; AID447991; AID447992; AID456795; AID463865; AID465153; AID478330; AID524995; AID539709; AID541653; AID608776; AID628430; AID723479; AID723726; AID769932; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Polyamine deacetylase HDAC10Homo sapiens (human)Ki0.17190.00000.76878.1900AID1479819; AID447579; AID487231
Histone deacetylase 11 Homo sapiens (human)IC50 (µMol)0.69890.00030.92989.9000AID1127332; AID1173704; AID1246513; AID1273502; AID1294969; AID1459975; AID1532639; AID1605948; AID1622926; AID1702070; AID1781513; AID1802451; AID1898913; AID242687; AID286454; AID316875; AID316888; AID331898; AID382342; AID417654; AID420326; AID447991; AID447992; AID456795; AID463865; AID478330; AID539709; AID541654; AID608776; AID628429; AID723460; AID723479; AID723726; AID769930; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 11 Homo sapiens (human)Ki0.45250.00011.21478.1900AID1479820; AID447579
Histone deacetylase 9Mus musculus (house mouse)IC50 (µMol)0.00140.00140.00140.0014AID90519
Histone deacetylase 7Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Histone deacetylase 6 Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Histone deacetylase 4Rattus norvegicus (Norway rat)IC50 (µMol)0.18540.00280.35173.5120AID242559; AID242560; AID242561; AID242586; AID242587; AID242600; AID90521; AID90522
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)1.29720.00070.99479.9000AID1127329; AID1173704; AID1246510; AID1254049; AID1273502; AID1276713; AID1280317; AID1294968; AID1354394; AID1363781; AID1384762; AID1394892; AID1459972; AID1529525; AID1532636; AID1586083; AID1605945; AID1622919; AID1647307; AID1651335; AID1690110; AID1702067; AID1758522; AID1765328; AID1781513; AID1802398; AID1802451; AID1833065; AID1862621; AID1863440; AID1901144; AID240720; AID242687; AID286454; AID316875; AID316888; AID331898; AID366643; AID367239; AID382342; AID408883; AID417651; AID420326; AID447991; AID447992; AID447995; AID456795; AID463865; AID465152; AID478330; AID488277; AID524996; AID539709; AID541647; AID568155; AID608776; AID611686; AID704015; AID723461; AID723479; AID723726; AID756021; AID769933; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 8Homo sapiens (human)Ki0.14050.00020.75258.1900AID1236445; AID1479813; AID1503585; AID447579; AID487228; AID496808; AID760388
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)0.25590.00000.53769.9000AID1127327; AID1173704; AID1173707; AID1246511; AID1254048; AID1273502; AID1276712; AID1280316; AID1294967; AID1322061; AID1322067; AID1324229; AID1363780; AID1384209; AID1384763; AID1394891; AID1401560; AID1424816; AID1432956; AID1459955; AID1473143; AID1518780; AID1525776; AID1528345; AID1529524; AID1530557; AID1532634; AID1557982; AID1586081; AID1591716; AID1605943; AID1622924; AID1622948; AID1647309; AID1651334; AID1659237; AID1690109; AID1709383; AID1758521; AID1764792; AID1765327; AID1781513; AID1802398; AID1802451; AID1833066; AID1862620; AID1863438; AID1882462; AID1895827; AID1901145; AID240719; AID242687; AID254794; AID269913; AID286454; AID308645; AID313187; AID316875; AID316888; AID331617; AID331898; AID331900; AID366644; AID367238; AID382342; AID408885; AID417649; AID420326; AID447991; AID447992; AID447996; AID456795; AID461093; AID463865; AID465154; AID478330; AID488276; AID524999; AID538409; AID539709; AID541652; AID568154; AID608776; AID611685; AID628433; AID695596; AID708215; AID723462; AID723479; AID723726; AID764212; AID769931; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 6Homo sapiens (human)Ki0.07300.00010.41568.1900AID1236450; AID1479812; AID331900; AID447579; AID487227; AID496806; AID760386
Histone deacetylase 9Homo sapiens (human)IC50 (µMol)0.57040.00050.94139.9000AID1127330; AID1173704; AID1246517; AID1273502; AID1578490; AID1622923; AID1781513; AID1802398; AID1802451; AID242687; AID286454; AID316875; AID316888; AID331898; AID382342; AID417652; AID420326; AID447991; AID447992; AID456795; AID463865; AID478330; AID524994; AID539709; AID541651; AID608776; AID628431; AID723479; AID723726; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 9Homo sapiens (human)Ki0.70130.00021.85209.0000AID1236449; AID447579; AID496809
Histone deacetylase 5Homo sapiens (human)IC50 (µMol)0.53320.00070.961010.0000AID1127326; AID1173704; AID1246515; AID1273502; AID1578488; AID1622921; AID1781513; AID1802398; AID1802451; AID242687; AID286454; AID316875; AID316888; AID331898; AID382342; AID417648; AID420326; AID447991; AID447992; AID456795; AID463865; AID478330; AID524998; AID539709; AID541649; AID608776; AID628434; AID723463; AID723479; AID723726; AID80353; AID90208; AID90211; AID90350; AID90351; AID90354; AID90528; AID90529
Histone deacetylase 5Homo sapiens (human)Ki1.28600.00021.29939.5000AID1236447; AID447579; AID496805; AID760385
Histone deacetylase Plasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)0.00060.00060.16880.9400AID414980
Nuclear receptor corepressor 2Homo sapiens (human)IC50 (µMol)0.01380.00170.59528.0000AID1294973; AID1363779; AID1532631; AID1622918; AID1647301; AID1901146; AID331899
Nuclear receptor corepressor 2Homo sapiens (human)Ki0.00050.00030.33253.2000AID1479815; AID331899
Histone deacetylase 6Mus musculus (house mouse)IC50 (µMol)0.03870.00060.20660.7870AID1182188; AID1390224; AID1622968; AID302799; AID309969; AID90519; AID90835
Histone deacetylase 5Mus musculus (house mouse)IC50 (µMol)0.01070.00140.01070.0200AID90519; AID90699
Histone deacetylase Zea maysIC50 (µMol)0.00040.00040.01330.0300AID273168; AID384316
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 4Homo sapiens (human)EC50 (µMol)2.50000.03002.35236.7000AID209973
Histone deacetylase 1Homo sapiens (human)EC50 (µMol)3.50000.03001.98776.7000AID208533; AID90679
Histone deacetylase 1Homo sapiens (human)Kd0.01370.01210.10490.2820AID1802399
Histone deacetylase 2Homo sapiens (human)Kd0.01370.01210.11300.2820AID1802399
Histone deacetylase 6Homo sapiens (human)EC50 (µMol)0.00520.00521.59986.7000AID1266100
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
unnamed protein productSaccharomyces cerevisiae (brewer's yeast)AC500.00080.00080.00080.0008AID463208
Histone deacetylase 3Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 3Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 4Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 4Homo sapiens (human)EC1000 (µMol)0.02000.02000.02000.0200AID461095
Histone deacetylase 4Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 1Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 1Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 7Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 7Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 2Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 2Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Polyamine deacetylase HDAC10Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Polyamine deacetylase HDAC10Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 11 Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 11 Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 8Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 8Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 6Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 6Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 9Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 9Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
Histone deacetylase 5Homo sapiens (human)AC500.40000.01002.70207.9000AID90344
Histone deacetylase 5Homo sapiens (human)Inhibition0.00350.00350.04170.0800AID243634
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (438)

Processvia Protein(s)Taxonomy
regulation of gene expressionLysine-specific demethylase 4EHomo sapiens (human)
chromatin remodelingLysine-specific demethylase 4EHomo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
establishment of mitotic spindle orientationHistone deacetylase 3Homo sapiens (human)
in utero embryonic developmentHistone deacetylase 3Homo sapiens (human)
positive regulation of protein phosphorylationHistone deacetylase 3Homo sapiens (human)
chromatin organizationHistone deacetylase 3Homo sapiens (human)
transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
protein deacetylationHistone deacetylase 3Homo sapiens (human)
regulation of mitotic cell cycleHistone deacetylase 3Homo sapiens (human)
positive regulation of protein ubiquitinationHistone deacetylase 3Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 3Homo sapiens (human)
positive regulation of TOR signalingHistone deacetylase 3Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
regulation of multicellular organism growthHistone deacetylase 3Homo sapiens (human)
positive regulation of protein import into nucleusHistone deacetylase 3Homo sapiens (human)
regulation of circadian rhythmHistone deacetylase 3Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 3Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 3Homo sapiens (human)
negative regulation of JNK cascadeHistone deacetylase 3Homo sapiens (human)
spindle assemblyHistone deacetylase 3Homo sapiens (human)
establishment of skin barrierHistone deacetylase 3Homo sapiens (human)
cellular response to fluid shear stressHistone deacetylase 3Homo sapiens (human)
positive regulation of cold-induced thermogenesisHistone deacetylase 3Homo sapiens (human)
DNA repair-dependent chromatin remodelingHistone deacetylase 3Homo sapiens (human)
cornified envelope assemblyHistone deacetylase 3Homo sapiens (human)
negative regulation of cardiac muscle cell differentiationHistone deacetylase 3Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
Factor XII activationPlasma kallikreinHomo sapiens (human)
proteolysisPlasma kallikreinHomo sapiens (human)
blood coagulationPlasma kallikreinHomo sapiens (human)
zymogen activationPlasma kallikreinHomo sapiens (human)
plasminogen activationPlasma kallikreinHomo sapiens (human)
fibrinolysisPlasma kallikreinHomo sapiens (human)
positive regulation of fibrinolysisPlasma kallikreinHomo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
response to hypoxiaCoagulation factor VIIHomo sapiens (human)
positive regulation of leukocyte chemotaxisCoagulation factor VIIHomo sapiens (human)
blood coagulationCoagulation factor VIIHomo sapiens (human)
circadian rhythmCoagulation factor VIIHomo sapiens (human)
response to carbon dioxideCoagulation factor VIIHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayCoagulation factor VIIHomo sapiens (human)
protein processingCoagulation factor VIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor VIIHomo sapiens (human)
positive regulation of cell migrationCoagulation factor VIIHomo sapiens (human)
animal organ regenerationCoagulation factor VIIHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor VIIHomo sapiens (human)
response to estradiolCoagulation factor VIIHomo sapiens (human)
response to vitamin KCoagulation factor VIIHomo sapiens (human)
response to genisteinCoagulation factor VIIHomo sapiens (human)
response to estrogenCoagulation factor VIIHomo sapiens (human)
positive regulation of positive chemotaxisCoagulation factor VIIHomo sapiens (human)
response to growth hormoneCoagulation factor VIIHomo sapiens (human)
response to cholesterolCoagulation factor VIIHomo sapiens (human)
response to thyroxineCoagulation factor VIIHomo sapiens (human)
response to Thyroid stimulating hormoneCoagulation factor VIIHomo sapiens (human)
response to 2,3,7,8-tetrachlorodibenzodioxineCoagulation factor VIIHomo sapiens (human)
response to astaxanthinCoagulation factor VIIHomo sapiens (human)
response to thyrotropin-releasing hormoneCoagulation factor VIIHomo sapiens (human)
proteolysisLeukotriene A-4 hydrolaseHomo sapiens (human)
lipid metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to zinc ionLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene biosynthetic processLeukotriene A-4 hydrolaseHomo sapiens (human)
protein metabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
peptide catabolic processLeukotriene A-4 hydrolaseHomo sapiens (human)
response to peptide hormoneLeukotriene A-4 hydrolaseHomo sapiens (human)
type I pneumocyte differentiationLeukotriene A-4 hydrolaseHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of DNA-templated transcriptionVitamin D3 receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
cell morphogenesisVitamin D3 receptorHomo sapiens (human)
skeletal system developmentVitamin D3 receptorHomo sapiens (human)
calcium ion transportVitamin D3 receptorHomo sapiens (human)
intracellular calcium ion homeostasisVitamin D3 receptorHomo sapiens (human)
lactationVitamin D3 receptorHomo sapiens (human)
negative regulation of cell population proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of gene expressionVitamin D3 receptorHomo sapiens (human)
negative regulation of keratinocyte proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D 24-hydroxylase activityVitamin D3 receptorHomo sapiens (human)
positive regulation of bone mineralizationVitamin D3 receptorHomo sapiens (human)
phosphate ion transmembrane transportVitamin D3 receptorHomo sapiens (human)
bile acid signaling pathwayVitamin D3 receptorHomo sapiens (human)
mRNA transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
positive regulation of keratinocyte differentiationVitamin D3 receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
decidualizationVitamin D3 receptorHomo sapiens (human)
intestinal absorptionVitamin D3 receptorHomo sapiens (human)
apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
positive regulation of apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
regulation of calcidiol 1-monooxygenase activityVitamin D3 receptorHomo sapiens (human)
mammary gland branching involved in pregnancyVitamin D3 receptorHomo sapiens (human)
vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
response to bile acidVitamin D3 receptorHomo sapiens (human)
multicellular organism developmentVitamin D3 receptorHomo sapiens (human)
cell differentiationVitamin D3 receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
positive regulation of gene expressionTissue factorHomo sapiens (human)
positive regulation of interleukin-8 productionTissue factorHomo sapiens (human)
positive regulation of endothelial cell proliferationTissue factorHomo sapiens (human)
activation of plasma proteins involved in acute inflammatory responseTissue factorHomo sapiens (human)
activation of blood coagulation via clotting cascadeTissue factorHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTissue factorHomo sapiens (human)
blood coagulationTissue factorHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor signaling pathwayTissue factorHomo sapiens (human)
protein processingTissue factorHomo sapiens (human)
positive regulation of cell migrationTissue factorHomo sapiens (human)
positive regulation of TOR signalingTissue factorHomo sapiens (human)
positive regulation of angiogenesisTissue factorHomo sapiens (human)
positive regulation of positive chemotaxisTissue factorHomo sapiens (human)
cytokine-mediated signaling pathwayTissue factorHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Bos taurus (cattle)
response to purine-containing compoundAdenosine receptor A1Bos taurus (cattle)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
chromatin remodelingHistone deacetylase 4Homo sapiens (human)
protein deacetylationHistone deacetylase 4Homo sapiens (human)
inflammatory responseHistone deacetylase 4Homo sapiens (human)
nervous system developmentHistone deacetylase 4Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 4Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 4Homo sapiens (human)
response to denervation involved in regulation of muscle adaptationHistone deacetylase 4Homo sapiens (human)
cardiac muscle hypertrophy in response to stressHistone deacetylase 4Homo sapiens (human)
protein sumoylationHistone deacetylase 4Homo sapiens (human)
B cell differentiationHistone deacetylase 4Homo sapiens (human)
positive regulation of protein sumoylationHistone deacetylase 4Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 4Homo sapiens (human)
B cell activationHistone deacetylase 4Homo sapiens (human)
regulation of protein bindingHistone deacetylase 4Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 4Homo sapiens (human)
negative regulation of glycolytic processHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 4Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 4Homo sapiens (human)
type I interferon-mediated signaling pathwayHistone deacetylase 4Homo sapiens (human)
response to interleukin-1Histone deacetylase 4Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
RNA splicing, via transesterification reactionsSplicing factor 3B subunit 3Homo sapiens (human)
mRNA splicing, via spliceosomeSplicing factor 3B subunit 3Homo sapiens (human)
regulation of DNA repairSplicing factor 3B subunit 3Homo sapiens (human)
RNA splicingSplicing factor 3B subunit 3Homo sapiens (human)
negative regulation of protein catabolic processSplicing factor 3B subunit 3Homo sapiens (human)
regulation of RNA splicingSplicing factor 3B subunit 3Homo sapiens (human)
positive regulation of DNA-templated transcriptionSplicing factor 3B subunit 3Homo sapiens (human)
U2-type prespliceosome assemblySplicing factor 3B subunit 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
base-excision repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
double-strand break repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatin remodelingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein deacetylationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of cell population proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
determination of adult lifespanNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
response to UVNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
retrotransposon silencingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of lipid metabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
pericentric heterochromatin formationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
subtelomeric heterochromatin formationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein destabilizationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of insulin secretionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of telomere maintenanceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
circadian regulation of gene expressionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of transcription elongation by RNA polymerase IINAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
ketone biosynthetic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of protein import into nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
glucose homeostasisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of circadian rhythmNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
post-translational protein modificationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of fat cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of gluconeogenesisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of gene expression, epigeneticNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of glycolytic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of glucose importNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of protein export from nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of fibroblast proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of protein secretionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of lipid catabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein delipidationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
cardiac muscle cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of cold-induced thermogenesisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of protein localization to chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of protein localization to chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
DNA repair-dependent chromatin remodelingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell population maintenanceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of chondrocyte proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of protein localization to plasma membraneNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of blood vessel branchingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein localization to site of double-strand breakNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of cellular senescenceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of double-strand break repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 7Homo sapiens (human)
vasculogenesisHistone deacetylase 7Homo sapiens (human)
chromatin remodelingHistone deacetylase 7Homo sapiens (human)
protein deacetylationHistone deacetylase 7Homo sapiens (human)
cell-cell junction assemblyHistone deacetylase 7Homo sapiens (human)
protein sumoylationHistone deacetylase 7Homo sapiens (human)
negative regulation of interleukin-2 productionHistone deacetylase 7Homo sapiens (human)
negative regulation of osteoblast differentiationHistone deacetylase 7Homo sapiens (human)
regulation of mRNA processingHistone deacetylase 7Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 7Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transductionHistone deacetylase 7Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
response to amphetamineHistone deacetylase 2Homo sapiens (human)
cardiac muscle hypertrophyHistone deacetylase 2Homo sapiens (human)
chromatin remodelingHistone deacetylase 2Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 2Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 2Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 2Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by competitive promoter bindingHistone deacetylase 2Homo sapiens (human)
negative regulation of neuron projection developmentHistone deacetylase 2Homo sapiens (human)
dendrite developmentHistone deacetylase 2Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 2Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 2Homo sapiens (human)
response to caffeineHistone deacetylase 2Homo sapiens (human)
heterochromatin formationHistone deacetylase 2Homo sapiens (human)
response to lipopolysaccharideHistone deacetylase 2Homo sapiens (human)
positive regulation of interleukin-1 productionHistone deacetylase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionHistone deacetylase 2Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 2Homo sapiens (human)
positive regulation of collagen biosynthetic processHistone deacetylase 2Homo sapiens (human)
cellular response to heatHistone deacetylase 2Homo sapiens (human)
response to nicotineHistone deacetylase 2Homo sapiens (human)
protein modification processHistone deacetylase 2Homo sapiens (human)
response to cocaineHistone deacetylase 2Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinHistone deacetylase 2Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 2Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 2Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-binding transcription factor activityHistone deacetylase 2Homo sapiens (human)
negative regulation of MHC class II biosynthetic processHistone deacetylase 2Homo sapiens (human)
positive regulation of proteolysisHistone deacetylase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 2Homo sapiens (human)
behavioral response to ethanolHistone deacetylase 2Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 2Homo sapiens (human)
response to hyperoxiaHistone deacetylase 2Homo sapiens (human)
hair follicle placode formationHistone deacetylase 2Homo sapiens (human)
negative regulation of dendritic spine developmentHistone deacetylase 2Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 2Homo sapiens (human)
fungiform papilla formationHistone deacetylase 2Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 2Homo sapiens (human)
cellular response to retinoic acidHistone deacetylase 2Homo sapiens (human)
cellular response to transforming growth factor beta stimulusHistone deacetylase 2Homo sapiens (human)
positive regulation of male mating behaviorHistone deacetylase 2Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 2Homo sapiens (human)
cellular response to dopamineHistone deacetylase 2Homo sapiens (human)
response to amyloid-betaHistone deacetylase 2Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 2Homo sapiens (human)
negative regulation of peptidyl-lysine acetylationHistone deacetylase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPolyamine deacetylase HDAC10Homo sapiens (human)
DNA repairPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationPolyamine deacetylase HDAC10Homo sapiens (human)
regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
macroautophagyPolyamine deacetylase HDAC10Homo sapiens (human)
positive regulation of mismatch repairPolyamine deacetylase HDAC10Homo sapiens (human)
homologous recombinationPolyamine deacetylase HDAC10Homo sapiens (human)
negative regulation of DNA-templated transcriptionPolyamine deacetylase HDAC10Homo sapiens (human)
polyamine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
spermidine deacetylationPolyamine deacetylase HDAC10Homo sapiens (human)
epigenetic regulation of gene expressionPolyamine deacetylase HDAC10Homo sapiens (human)
chromatin organizationHistone deacetylase 11 Homo sapiens (human)
oligodendrocyte developmentHistone deacetylase 11 Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 11 Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 9Homo sapiens (human)
negative regulation of cytokine productionHistone deacetylase 9Homo sapiens (human)
response to amphetamineHistone deacetylase 9Homo sapiens (human)
inflammatory responseHistone deacetylase 9Homo sapiens (human)
heart developmentHistone deacetylase 9Homo sapiens (human)
neuron differentiationHistone deacetylase 9Homo sapiens (human)
B cell differentiationHistone deacetylase 9Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 9Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 9Homo sapiens (human)
B cell activationHistone deacetylase 9Homo sapiens (human)
cholesterol homeostasisHistone deacetylase 9Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 9Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 9Homo sapiens (human)
regulation of skeletal muscle fiber developmentHistone deacetylase 9Homo sapiens (human)
regulation of striated muscle cell differentiationHistone deacetylase 9Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 9Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
inflammatory responseHistone deacetylase 5Homo sapiens (human)
response to xenobiotic stimulusHistone deacetylase 5Homo sapiens (human)
regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 5Homo sapiens (human)
response to activityHistone deacetylase 5Homo sapiens (human)
neuron differentiationHistone deacetylase 5Homo sapiens (human)
B cell differentiationHistone deacetylase 5Homo sapiens (human)
cellular response to insulin stimulusHistone deacetylase 5Homo sapiens (human)
B cell activationHistone deacetylase 5Homo sapiens (human)
response to cocaineHistone deacetylase 5Homo sapiens (human)
regulation of protein bindingHistone deacetylase 5Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 5Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 5Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityHistone deacetylase 5Homo sapiens (human)
cellular response to lipopolysaccharideHistone deacetylase 5Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisHistone deacetylase 5Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor corepressor 2Homo sapiens (human)
lactationNuclear receptor corepressor 2Homo sapiens (human)
response to organonitrogen compoundNuclear receptor corepressor 2Homo sapiens (human)
regulation of cellular ketone metabolic processNuclear receptor corepressor 2Homo sapiens (human)
cerebellum developmentNuclear receptor corepressor 2Homo sapiens (human)
response to estradiolNuclear receptor corepressor 2Homo sapiens (human)
estrous cycleNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayNuclear receptor corepressor 2Homo sapiens (human)
negative regulation of miRNA transcriptionNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (150)

Processvia Protein(s)Taxonomy
metal ion bindingLysine-specific demethylase 4EHomo sapiens (human)
histone H3K9me2/H3K9me3 demethylase activityLysine-specific demethylase 4EHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific demethylase 4EHomo sapiens (human)
histone deacetylase activityHistone deacetylase 1Mus musculus (house mouse)
transcription corepressor bindingHistone deacetylase 3Homo sapiens (human)
chromatin bindingHistone deacetylase 3Homo sapiens (human)
transcription corepressor activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase activityHistone deacetylase 3Homo sapiens (human)
protein bindingHistone deacetylase 3Homo sapiens (human)
enzyme bindingHistone deacetylase 3Homo sapiens (human)
cyclin bindingHistone deacetylase 3Homo sapiens (human)
chromatin DNA bindingHistone deacetylase 3Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 3Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 3Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 3Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 3Homo sapiens (human)
protein decrotonylase activityHistone deacetylase 3Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 3Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 3Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
serine-type endopeptidase activityPlasma kallikreinHomo sapiens (human)
protein bindingPlasma kallikreinHomo sapiens (human)
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
serine-type endopeptidase activityCoagulation factor VIIHomo sapiens (human)
signaling receptor bindingCoagulation factor VIIHomo sapiens (human)
calcium ion bindingCoagulation factor VIIHomo sapiens (human)
protein bindingCoagulation factor VIIHomo sapiens (human)
serine-type peptidase activityCoagulation factor VIIHomo sapiens (human)
RNA bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
epoxide hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
leukotriene-A4 hydrolase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
protein bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
peptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
zinc ion bindingLeukotriene A-4 hydrolaseHomo sapiens (human)
tripeptide aminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
metalloaminopeptidase activityLeukotriene A-4 hydrolaseHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
DNA-binding transcription factor activityVitamin D3 receptorHomo sapiens (human)
vitamin D response element bindingVitamin D3 receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificVitamin D3 receptorHomo sapiens (human)
DNA bindingVitamin D3 receptorHomo sapiens (human)
nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
protein bindingVitamin D3 receptorHomo sapiens (human)
zinc ion bindingVitamin D3 receptorHomo sapiens (human)
bile acid nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
nuclear retinoid X receptor bindingVitamin D3 receptorHomo sapiens (human)
calcitriol bindingVitamin D3 receptorHomo sapiens (human)
lithocholic acid bindingVitamin D3 receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingVitamin D3 receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
serine-type endopeptidase activityTissue factorHomo sapiens (human)
protease bindingTissue factorHomo sapiens (human)
protein bindingTissue factorHomo sapiens (human)
phospholipid bindingTissue factorHomo sapiens (human)
cytokine receptor activityTissue factorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 4Homo sapiens (human)
histone bindingHistone deacetylase 4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase activityHistone deacetylase 4Homo sapiens (human)
protein bindingHistone deacetylase 4Homo sapiens (human)
zinc ion bindingHistone deacetylase 4Homo sapiens (human)
SUMO transferase activityHistone deacetylase 4Homo sapiens (human)
potassium ion bindingHistone deacetylase 4Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 4Homo sapiens (human)
identical protein bindingHistone deacetylase 4Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 4Homo sapiens (human)
molecular adaptor activityHistone deacetylase 4Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 4Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
protein bindingSplicing factor 3B subunit 3Homo sapiens (human)
protein-containing complex bindingSplicing factor 3B subunit 3Homo sapiens (human)
U2 snRNA bindingSplicing factor 3B subunit 3Homo sapiens (human)
chromatin bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
damaged DNA bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
zinc ion bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleotidyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatin DNA bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleosome bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein homodimerization activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K9 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+ bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K18 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+-protein-arginine ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
DNA damage sensor activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K56 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein demyristoylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein depalmitoylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+- protein-lysine ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
TORC2 complex bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
transcription corepressor activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatin bindingHistone deacetylase 7Homo sapiens (human)
transcription corepressor activityHistone deacetylase 7Homo sapiens (human)
histone deacetylase activityHistone deacetylase 7Homo sapiens (human)
protein kinase C bindingHistone deacetylase 7Homo sapiens (human)
protein bindingHistone deacetylase 7Homo sapiens (human)
SUMO transferase activityHistone deacetylase 7Homo sapiens (human)
protein kinase bindingHistone deacetylase 7Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 7Homo sapiens (human)
metal ion bindingHistone deacetylase 7Homo sapiens (human)
14-3-3 protein bindingHistone deacetylase 7Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 7Homo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 2Homo sapiens (human)
chromatin bindingHistone deacetylase 2Homo sapiens (human)
RNA bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase activityHistone deacetylase 2Homo sapiens (human)
protein bindingHistone deacetylase 2Homo sapiens (human)
enzyme bindingHistone deacetylase 2Homo sapiens (human)
heat shock protein bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 2Homo sapiens (human)
histone bindingHistone deacetylase 2Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 2Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 2Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 2Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 2Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activityHistone deacetylase 2Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 2Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
protein bindingPolyamine deacetylase HDAC10Homo sapiens (human)
zinc ion bindingPolyamine deacetylase HDAC10Homo sapiens (human)
deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
enzyme bindingPolyamine deacetylase HDAC10Homo sapiens (human)
protein lysine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase bindingPolyamine deacetylase HDAC10Homo sapiens (human)
acetylputrescine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
acetylspermidine deacetylase activityPolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase activityHistone deacetylase 11 Homo sapiens (human)
protein bindingHistone deacetylase 11 Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 11 Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein kinase C bindingHistone deacetylase 9Homo sapiens (human)
protein bindingHistone deacetylase 9Homo sapiens (human)
histone H3K14 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H3K9 deacetylase activityHistone deacetylase 9Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone H4K16 deacetylase activityHistone deacetylase 9Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 9Homo sapiens (human)
metal ion bindingHistone deacetylase 9Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 9Homo sapiens (human)
transcription cis-regulatory region bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 5Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 5Homo sapiens (human)
chromatin bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase activityHistone deacetylase 5Homo sapiens (human)
protein kinase C bindingHistone deacetylase 5Homo sapiens (human)
protein bindingHistone deacetylase 5Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 5Homo sapiens (human)
identical protein bindingHistone deacetylase 5Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 5Homo sapiens (human)
metal ion bindingHistone deacetylase 5Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 5Homo sapiens (human)
DNA bindingNuclear receptor corepressor 2Homo sapiens (human)
chromatin bindingNuclear receptor corepressor 2Homo sapiens (human)
transcription corepressor activityNuclear receptor corepressor 2Homo sapiens (human)
Notch bindingNuclear receptor corepressor 2Homo sapiens (human)
protein bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
histone deacetylase bindingNuclear receptor corepressor 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor corepressor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (98)

Processvia Protein(s)Taxonomy
nucleusLysine-specific demethylase 4EHomo sapiens (human)
nucleoplasmLysine-specific demethylase 4EHomo sapiens (human)
chromatinLysine-specific demethylase 4EHomo sapiens (human)
nucleusLysine-specific demethylase 4EHomo sapiens (human)
nucleoplasmHistone deacetylase 1Mus musculus (house mouse)
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Homo sapiens (human)
cytoplasmHistone deacetylase 3Homo sapiens (human)
Golgi apparatusHistone deacetylase 3Homo sapiens (human)
cytosolHistone deacetylase 3Homo sapiens (human)
plasma membraneHistone deacetylase 3Homo sapiens (human)
mitotic spindleHistone deacetylase 3Homo sapiens (human)
histone deacetylase complexHistone deacetylase 3Homo sapiens (human)
transcription repressor complexHistone deacetylase 3Homo sapiens (human)
nucleusHistone deacetylase 3Homo sapiens (human)
nucleoplasmHistone deacetylase 3Mus musculus (house mouse)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionPlasma kallikreinHomo sapiens (human)
extracellular spacePlasma kallikreinHomo sapiens (human)
plasma membranePlasma kallikreinHomo sapiens (human)
extracellular exosomePlasma kallikreinHomo sapiens (human)
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular regionCoagulation factor VIIHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor VIIHomo sapiens (human)
Golgi lumenCoagulation factor VIIHomo sapiens (human)
plasma membraneCoagulation factor VIIHomo sapiens (human)
vesicleCoagulation factor VIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor VIIHomo sapiens (human)
serine-type peptidase complexCoagulation factor VIIHomo sapiens (human)
extracellular spaceCoagulation factor VIIHomo sapiens (human)
extracellular regionLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleoplasmLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
extracellular exosomeLeukotriene A-4 hydrolaseHomo sapiens (human)
tertiary granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
ficolin-1-rich granule lumenLeukotriene A-4 hydrolaseHomo sapiens (human)
cytosolLeukotriene A-4 hydrolaseHomo sapiens (human)
nucleusLeukotriene A-4 hydrolaseHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
nucleusVitamin D3 receptorHomo sapiens (human)
nucleusVitamin D3 receptorHomo sapiens (human)
nucleoplasmVitamin D3 receptorHomo sapiens (human)
cytosolVitamin D3 receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexVitamin D3 receptorHomo sapiens (human)
chromatinVitamin D3 receptorHomo sapiens (human)
receptor complexVitamin D3 receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
extracellular spaceTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
external side of plasma membraneTissue factorHomo sapiens (human)
cell surfaceTissue factorHomo sapiens (human)
membraneTissue factorHomo sapiens (human)
collagen-containing extracellular matrixTissue factorHomo sapiens (human)
serine-type peptidase complexTissue factorHomo sapiens (human)
plasma membraneTissue factorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
nucleusHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 4Homo sapiens (human)
cytoplasmHistone deacetylase 4Homo sapiens (human)
cytosolHistone deacetylase 4Homo sapiens (human)
nuclear speckHistone deacetylase 4Homo sapiens (human)
histone deacetylase complexHistone deacetylase 4Homo sapiens (human)
chromatinHistone deacetylase 4Homo sapiens (human)
transcription repressor complexHistone deacetylase 4Homo sapiens (human)
nucleoplasmHistone deacetylase 2Mus musculus (house mouse)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
SAGA complexSplicing factor 3B subunit 3Homo sapiens (human)
nucleusSplicing factor 3B subunit 3Homo sapiens (human)
nucleoplasmSplicing factor 3B subunit 3Homo sapiens (human)
spliceosomal complexSplicing factor 3B subunit 3Homo sapiens (human)
U2-type spliceosomal complexSplicing factor 3B subunit 3Homo sapiens (human)
U2 snRNPSplicing factor 3B subunit 3Homo sapiens (human)
nucleolusSplicing factor 3B subunit 3Homo sapiens (human)
U12-type spliceosomal complexSplicing factor 3B subunit 3Homo sapiens (human)
U2-type precatalytic spliceosomeSplicing factor 3B subunit 3Homo sapiens (human)
catalytic step 2 spliceosomeSplicing factor 3B subunit 3Homo sapiens (human)
nucleusSplicing factor 3B subunit 3Homo sapiens (human)
nucleoplasmHistone deacetylase 1Rattus norvegicus (Norway rat)
nucleoplasmHistone deacetylase 4Mus musculus (house mouse)
nucleoplasmHistone deacetylase 3Rattus norvegicus (Norway rat)
nucleolusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
pericentric heterochromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
endoplasmic reticulumNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
site of double-strand breakNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
site of DNA damageNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleoplasmNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
intracellular membrane-bounded organelleNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromosome, subtelomeric regionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleusHistone deacetylase 7Homo sapiens (human)
nucleoplasmHistone deacetylase 7Homo sapiens (human)
cytoplasmHistone deacetylase 7Homo sapiens (human)
cytosolHistone deacetylase 7Homo sapiens (human)
chromosome, telomeric regionHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleoplasmHistone deacetylase 2Homo sapiens (human)
cytoplasmHistone deacetylase 2Homo sapiens (human)
NuRD complexHistone deacetylase 2Homo sapiens (human)
Sin3-type complexHistone deacetylase 2Homo sapiens (human)
histone deacetylase complexHistone deacetylase 2Homo sapiens (human)
chromatinHistone deacetylase 2Homo sapiens (human)
protein-containing complexHistone deacetylase 2Homo sapiens (human)
ESC/E(Z) complexHistone deacetylase 2Homo sapiens (human)
nucleusHistone deacetylase 2Homo sapiens (human)
nucleusPolyamine deacetylase HDAC10Homo sapiens (human)
nucleoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytoplasmPolyamine deacetylase HDAC10Homo sapiens (human)
cytosolPolyamine deacetylase HDAC10Homo sapiens (human)
intracellular membrane-bounded organellePolyamine deacetylase HDAC10Homo sapiens (human)
histone deacetylase complexPolyamine deacetylase HDAC10Homo sapiens (human)
nucleusHistone deacetylase 11 Homo sapiens (human)
plasma membraneHistone deacetylase 11 Homo sapiens (human)
histone deacetylase complexHistone deacetylase 11 Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
nucleusHistone deacetylase 9Homo sapiens (human)
nucleoplasmHistone deacetylase 9Homo sapiens (human)
cytoplasmHistone deacetylase 9Homo sapiens (human)
histone deacetylase complexHistone deacetylase 9Homo sapiens (human)
transcription regulator complexHistone deacetylase 9Homo sapiens (human)
histone methyltransferase complexHistone deacetylase 9Homo sapiens (human)
nucleusHistone deacetylase 5Homo sapiens (human)
nucleoplasmHistone deacetylase 5Homo sapiens (human)
cytoplasmHistone deacetylase 5Homo sapiens (human)
Golgi apparatusHistone deacetylase 5Homo sapiens (human)
cytosolHistone deacetylase 5Homo sapiens (human)
nuclear speckHistone deacetylase 5Homo sapiens (human)
histone deacetylase complexHistone deacetylase 5Homo sapiens (human)
nucleusNuclear receptor corepressor 2Homo sapiens (human)
nucleoplasmNuclear receptor corepressor 2Homo sapiens (human)
membraneNuclear receptor corepressor 2Homo sapiens (human)
nuclear matrixNuclear receptor corepressor 2Homo sapiens (human)
nuclear bodyNuclear receptor corepressor 2Homo sapiens (human)
chromatinNuclear receptor corepressor 2Homo sapiens (human)
transcription repressor complexNuclear receptor corepressor 2Homo sapiens (human)
cytosolHistone deacetylase 6Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1101)

Assay IDTitleYearJournalArticle
AID90677Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID1532634Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using RHKK-Ac as substrate by fluorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID1394889Inhibition of human HDAC1 using RHKK(Ac) as substrate2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID385445Effect on TNF-alpha-induced TFkappaB activation assessed as p65/p50 binding to TFkappaB in HUVEC preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID300678Antiproliferative activity against H661 cells after 48 hrs by XTT assay2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis and biological evaluation of 1,4-benzodiazepine-2,5-dione-based HDAC inhibitors.
AID755476Inhibition of recombinant human HDAC7 using acetyl-Lys-(trifluoroacetyl)-AMC as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID1622916Inhibition of recombinant full-length human HDAC1 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1324229Inhibition of HDAC6 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID1384765Selectivity index, ratio of IC50 for human HDAC2 to IC50 for human HDAC62018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID1595394Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 500 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control2019European journal of medicinal chemistry, Jun-15, Volume: 172Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability.
AID1401640Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1628751Antiproliferative activity against human SK-BR-3 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1294970Inhibition of human recombinant HDAC9 using trifluoroacetyl lysine as substrate2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1127328Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID488357Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1322061Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID764213Inhibition of human recombinant HDAC4 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID1758522Inhibition of human recombinant HDAC8 using [RHKK(Ac)] fluorogenic substrate2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID1622925Inhibition of recombinant full-length human HDAC10 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1647308Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using Boc-K(Ac)-AMC as substrate after 90 mins by fluorimetry analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1156707Cytotoxicity against human MOLT4 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID446381Inhibition of SIRT2 in human MCF7 cells assessed as tubulin hyperacetylation at 0.1 uM after 16 hrs by Western blot2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
AID1853418Inhibition of human MMP-8 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID1384758Inhibition of human HDAC10 using RHKKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID1628763Antiproliferative activity against human PC3 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID367241Selectivity ratio of IC50 for human recombinant histone deacetylase 8 to IC50 for human recombinant histone deacetylase 62009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID525025Inhibition of HDAC in human CFBE41o- cell line assessed as increase in CFTR mRNA at 0.1 uM by RT-PCR2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1702070Inhibition of human full length HDAC11 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID50586Inhibitory concentration against colon HCT116 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID156319Inhibitory activity against PC-3 cell line2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
QSAR studies of PC-3 cell line inhibition activity of TSA and SAHA-like hydroxamic acids.
AID1401593Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID90346Ability to inhibit recombinant human histone deacetylase 1 (HDAC-1); Potent inhibitor2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
(2-amino-phenyl)-amides of omega-substituted alkanoic acids as new histone deacetylase inhibitors.
AID1529528Antiproliferative activity against human K562 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID516284Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH412 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID90662Inhibition against partially purified human histone deacetylase 1 (HDAC-1)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID1401632Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1155332Inhibition of HDAC in Plasmodium falciparum 3D7 trophozoites assessed as histone H4 hyperacetylation level at 500 nM after 3 hrs by Western blotting analysis relative to control2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID385450Inhibition of IL-1-beta-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of IL1-beta challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1363777Inhibition of C-terminal FLAG-His-tagged full length recombinant human HDAC1 expressed in Sf21 insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID1387537Inhibition of mouse HDAC6 expressed in 293T cells at 100 uM using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay relative to control2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.
AID1363779Inhibition of recombinant human HDAC3/NCOR2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID1384759Inhibition of human HDAC1 using RHKKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID1459971Inhibition of recombinant human HDAC7 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1863433Inhibition of HDAC1 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID503117Induction of p21 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting2007Nature chemical biology, Sep, Volume: 3, Issue:9
Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA.
AID1431818Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1862613Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID366644Inhibition of HDAC6 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID723728Cytotoxicity against cisplatin resistant human A2780 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID90838Tested for inhibition of Histone deacetylase 6 induced acetylated tubulin in mammalian cells.2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID324484Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID324380Induction of light chain 3-GFP level in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID43027Cytotoxicity of compound against normal human ovarian C18013S cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1656940Cytotoxicity against human HepG2 cells assessed as reduction in cell viability
AID90354Inhibitory concentration against human histone deacetylase (HDAC)2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1173707Inhibition of HDAC6 (unknown origin) after 15 mins by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Aurones as histone deacetylase inhibitors: identification of key features.
AID358673Induction of REST/NRSF-coupled repression of luciferase tagged rat RE1/NRSE BDNF promoter activity expressed in ST14A cells at 75 nM assessed as increase in luciferase activity2007The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators.
AID1529535Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1833068Selectivity ratio of IC50 for full length recombinant C-terminal GST-fusion-tagged human HDAC2 to IC50 for full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID230221Inhibitory concentration against HDAC6/HDAC12003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID90695Inhibition of maize Histone deacetylase 2 (HD-2) activity1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.
AID1589335Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate at 50 uM by fluorescence assay relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.
AID769933Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1862615Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1862608Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1236441Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay2015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1127327Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1622966Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID408886Selectivity for HDAC6 over HDAC12008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1765332Selectivity index, ratio of IC50 for human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID628435Inhibition of human recombinant HDAC4 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1401636Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID723464Inhibition of human HDAC4 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID408887Selectivity for HDAC10 over HDAC12008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID503530Inhibition of HDAC in human GM15850 cells assessed as increase in total acetylated histone level at 0.1 uM after 12 hrs by Western blot analysis2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID408882Inhibition of HDAC32008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1127326Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1529532Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1586078Inhibition of human HDAC2 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID90840Inhibitory activity against histone deacetylase 8 prepared from mouse melanoma B16/BL6 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
AID1394891Inhibition of human HDAC6 using RHKK(Ac) as substrate2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID417069Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Psammaplin A as a general activator of cell-based signaling assays via HDAC inhibition and studies on some bromotyrosine derivatives.
AID1532656Antiangiogenic activity in zebrafish embryo assessed as effect on blood vessel development at 10 uM administered from 24 to 50 hrs post fertilization for 24 hrs and measured after 72 hrs by alkaline phosphatase assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID670032Inhibition of Class 1 histone deacetylase in human MCF7 cells assessed as up-regulation of p21 protein level at 0.5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID324432Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID524996Inhibition of HDAC8 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1363780Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID654541Inhibition of human HDAC1 after 30 mins by fluorescence assay2012Journal of natural products, Feb-24, Volume: 75, Issue:2
Trichostatin analogues JBIR-109, JBIR-110, and JBIR-111 from the marine sponge-derived Streptomyces sp. RM72.
AID1578490Inhibition of recombinant human HDAC9 (604-1066 residues) expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1177040Cytotoxicity against human LO2 cells after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID551713Inhibition of HDAC by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Design and synthesis of aryl ether and sulfone hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
AID1557982Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by s2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
AID417649Inhibition of human HDAC62009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID1758525Selectivity ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC62021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID1459973Inhibition of recombinant human HDAC9 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1260640Inhibition of human recombinant HDAC4 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID456799Cytotoxicity against african green monkey Vero cells after 1 to 2 days by neutral red assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID683274Inhibition of HDAC1 by fluorometric assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects.
AID1781512Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID1622918Inhibition of recombinant full-length human HDAC3/NCOR2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1394892Inhibition of human HDAC8 using RHKAcKAc as substrate2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1156703Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID90338Tested for inhibitory concentration required to inhibit 50% of histone deacetylase (HDAC) from human T cell leukemia Jurkat cell2002Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10
Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group.
AID519598Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-sensitive Plasmodium falciparum 3D72008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1605942Inhibition of recombinant human C-terminal His-fusion tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1833064Inhibition of full length recombinant C-terminal GST-fusion-tagged human HDAC2 expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID541646Inhibition of human HDAC3 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1651337Selectivity ratio of IC50 for recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells to IC50 of human HDAC62020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID1401622Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID350020Antiproliferative activity against human NCI-H661 cells after 48 hrs by XTT assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.
AID1532636Inhibition of recombinant C-terminal His-tagged human HDAC8 (1 to 377 residues) expressed in Baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID316882Growth inhibition of human neonatal foreskin fibroblasts cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID456795Inhibition of HDAC in human HeLa cell nuclear extracts after 15 mins by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID308643Inhibition of human HDAC12007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1423502Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of NAM by fluorescence-based SDS-denaturation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID1421905Cytotoxicity against human NFF cells2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID487226Inhibition of recombinant HDAC32010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID487231Inhibition of HDAC102010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID90680Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID1764791Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1459954Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID417651Inhibition of human HDAC82009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID299644Increase in GRP78 protein level in HEK293 cells at 600 nM by immunoblot2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition.
AID385470Effect on TNF-alpha-induced NF-kappaB activation assessed as p65/p50 binding to NF-kappaB in HUVEC at 0.3 uM preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1630623Inhibition of recombinant C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1210092Increase in NAT1 enzyme activity in 100% confluent human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1628760Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1557981Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mi2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
AID90691Inhibition of maize Histone deacetylase 22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID764212Inhibition of human recombinant HDAC6 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID524999Inhibition of HDAC6 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID385465Induction of PMA-induced TFkappaB-dependent wild type tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1901144Inhibition of human full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell using fluorogenic HDAC class 2a substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1622921Inhibition of recombinant full-length human HDAC5 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1276712Inhibition of recombinant human HDAC6 by fluorimetry2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.
AID1177041Cytotoxicity against human HEK293 cells after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID80353Concentration required to inhibit the partially purified HDAC enzyme by 50% obtained from H1299 cell lysate2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1709383Inhibition of recombinant human full-length N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected Sf9 insect cells using RHKK(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1401602Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID723460Inhibition of human HDAC11 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID420318Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1182190Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID1459955Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1529510Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID417646Inhibition of human HDAC32009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID143656Cytotoxicity of compound against normal human normal neonatal foreskin fibroblasts (NFF)2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID704015Inhibition of human recombinant HDAC8 using fluor de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 25 mins by microplate reader analysis2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.
AID447996Inhibition of human recombinant HDAC6 after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID507021Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay2007Nature chemical biology, Sep, Volume: 3, Issue:9
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
AID1628750Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID331898Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from HDAC in human HeLa nuclear cell extract by fluorescence p2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID1401608Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID652766Induction of CFTR deltaF508 mutant protein expression in cystic fibrosis patient lung cells relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID385446Inhibition of LPS-induced tissue factor activity in human PBMC preincubated for 4 hrs assessed after 5 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1690107Inhibition of recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorimetry analysis2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID1173704Inhibition of HDAC in human HeLa cell extract after 15 mins by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Aurones as histone deacetylase inhibitors: identification of key features.
AID611684Inhibition of human HDAC2 using rhodamine as substrate after 1 hrs by fluorescence assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
AID465154Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1384209Inhibition of HDAC6 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1401557Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1901151Inhibition of recombinant human N-terminal GST-fused/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC class 2a substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID1401633Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1479817Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID360096Inhibition of IL-1-beta-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of IL1-beta challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1764788Inhibition of HDAC6 in mouse Neuro2a cells assessed as fold increase in ratio of acetylated alpha-tubulin to alpha tubulin at 1 uM incubated for overnight by Western blot analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID456796Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID1898913Inhibition of HDAC11 (unknown origin) using fluorogenic peptide 382 RHKK(Ac)AM as substrate and measured by fluorescence assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Antitumor activity of novel POLA1-HDAC11 dual inhibitors.
AID1578491Inhibition of recombinant full length human HDAC10 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID628429Inhibition of human recombinant HDAC11 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID201971Cytotoxicity of compound against normal human melanoma SK-MEL-28 cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1155333Inhibition of histone deacetylase in Plasmodium falciparum nuclear lysates at 1 uM by fluorescence assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID566552Inhibition of HDAC in human HeLa cells at 1 uM after 10 mins by fluorometric assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID516295Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH444 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1294967Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate incubated for 90 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1591717Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1690109Inhibition of recombinant human HDAC6 using RHK-K(Ac)-AMC as substrate by fluorescence based assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID538408Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID1260638Inhibition of human recombinant HDAC2 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID628431Inhibition of human recombinant HDAC9 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1431817Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1431813Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1127323Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID695596Inhibition of HDAC6 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID90529Inhibitory concentration against histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID496807Inhibition of human HDAC72010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1401598Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1605959Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluo2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID8297Inhibitory concentration required to reduce A549 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID1459970Inhibition of recombinant human HDAC5 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1532646Selectivity ratio of IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) to IC50 for recombinant C-terminal His-tagged human HDAC8 (1 to 377 residues)2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID385434Inhibition of LPS-induced tissue factor activity in HUVEC at 0.3 uM preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1532640Selectivity ratio of IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 (1 to 482 residues) to IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues)2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID1656941Cytotoxicity against human A2058 cells assessed as reduction in cell viability
AID1758520Inhibition of human recombinant HDAC3 using [RHKK(Ac)] fluorogenic substrate2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID568155Inhibition of HDAC8 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID1384762Inhibition of human HDAC8 using RHKAcKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID408885Inhibition of HDAC62008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1479811Inhibition of full length recombinant human C-terminal GST-tagged HDAC2 expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID90520Inhibition of in vitro enzyme activity measured in partially purified rat liver Histone deacetylase preparation2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID519597Selectivity index, ratio of IC50 for neonatal foreskin fibroblasts to IC50 for chloroquine-resistant Plasmodium falciparum Dd22008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1127324Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1127330Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1280314Inhibition of human KDAC1 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1503585Inhibition of C-terminal His-tagged human recombinant full-length HDAC8 expressed in baculovirus expression system assessed as reduction in 7-amino-4-methylcoumarin by fluorescence based assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design.
AID420317Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID461092Inhibition of HDAC42010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
AID755477Inhibition of recombinant human HDAC6 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID102521Inhibitory concentration against lung H446 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID659293Inhibition of HDAC2 in human HeLa cell nuclear extracts in presence of dithiothreitol by HDAC fluorescent assay2012European journal of medicinal chemistry, Jun, Volume: 52A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study.
AID756006Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Cdh1 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1863437Inhibition of HDAC5 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1622948Inhibition of human HDAC6 using fluorogenic HDAC substrate2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1765331Selectivity index, ratio of IC50 for human recombinant full length HDAC6 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1622923Inhibition of recombinant full-length human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1863438Inhibition of HDAC6 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1605950Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID417645Inhibition of human HDAC22009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID447579Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.
AID1647307Inhibition of recombinant C-terminal His-tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorescence assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1765326Inhibition of human full-length recombinant HDAC3 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1236443Inhibition of human HDAC22015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1656944Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability
AID1863434Inhibition of HDAC2 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID650229Inhibition of HDAC12012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1276706Inhibition of recombinant human HDAC2 by fluorimetry2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.
AID755480Inhibition of recombinant human HDAC2 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID503115Induction of p16 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting2007Nature chemical biology, Sep, Volume: 3, Issue:9
Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA.
AID1628746Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1363778Inhibition of C-terminal GST-tagged recombinant human HDAC2 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID420326Inhibition of HDAC from human HeLa cells by fluorogenic enzyme assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1401630Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID496806Inhibition of human HDAC62010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID90661In vitro inhibition of partially purified recombinant human Histone deacetylase 12001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Design and synthesis of a novel class of histone deacetylase inhibitors.
AID316875Inhibition of HDAC from human HeLa cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1246510Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID568153Inhibition of HDAC4 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID525021Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 5 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1294973Inhibition of full length human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/human recombinant N-terminal GST-tagged NCOR2 expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1622992Antiproliferative activity against human MCF7 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1246508Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1765324Inhibition of human full-length recombinant HDAC1 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1260641Inhibition of human recombinant HDAC5 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID605941Cytostatic activity against human DMS53 cells assessed as inhibition of cell proliferation after 2 days by MTT assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Microbial transformation of trichostatin A to 2,3-dihydrotrichostatin A.
AID385452Inhibition of baseline tissue factor activity in non-stimulated C57BL/6J mouse macrophages after 4 hrs by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1177038Cytotoxicity against human HepG2 cells after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID516317Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate RB3 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID43458Inhibitory concentration against breast MCF-7 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1390226Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B-based colorimetric assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.
AID420325Inhibition of HDAC1 in human NIH3T3 cells by radiometric histone deacetylation assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1441700Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1401600Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID273168Inhibition of maize HD1B2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1384767Selectivity index, ratio of IC50 for human HDAC8 to IC50 for human HDAC62018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID723726Inhibition of HDAC in human A2780 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1853420Inhibition of human TACE at 0.5 uM by fluorescence based assay2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID104356Cytotoxicity against human melanoma MM96L cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1156708Cytotoxicity against human U937 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID1354369Antiproliferative activity against human HL60 cells after 24 hrs by MTT assay
AID723462Inhibition of human HDAC6 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID488277Inhibition of HDAC82010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1647302Inhibition of recombinant N-terminal GST-tagged/C-terminal His-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1586081Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID90199Experimental anti-HDAC (anti-histone deacetylase) activity of the compound2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors.
AID1862621Inhibition of HDAC8 (unknown origin) measured by fluorometry assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1605948Inhibition of human recombinant N-terminal Streptavidin2-tagged HDAC11 (1 to 347 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1431811Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID90681Inhibition of mouse HDAC12004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID487228Inhibition of recombinant HDAC82010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID568150Inhibition of HDAC1 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID1702063Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 (627 to 1084 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID382113Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH reporter assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy.
AID756008Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Sox2 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID105452Inhibitory concentration required to reduce MDAmb 231 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID756023Inhibition of HDAC2 (unknown origin) after 30 mins by fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID143655Cytotoxicity of compound against human normal neonatal foreskin fibroblasts (NFF) cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1758524Selectivity ratio of IC50 for human recombinant HDAC3 to IC50 for human recombinant HDAC62021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID360090Effect on TNF-alpha-induced increase in HDAC3 binding to TFkappaB in HUVEC cells at preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1702065Inhibition of recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID659292Inhibition of human HDAC1 in presence of dithiothreitol by HDAC fluorescent assay2012European journal of medicinal chemistry, Jun, Volume: 52A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study.
AID1324226Inhibition of HDAC1 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID360094Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID723466Inhibition of human HDAC1 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1293877Competitive inhibition of HDAC in human HeLa nuclear cells at 10 to 25 uM using Boc-acetyl-lysine-AMC as substrate after 30 mins by Lineweaver-Burk plot analysis2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID1595395Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 50 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control2019European journal of medicinal chemistry, Jun-15, Volume: 172Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability.
AID1630622Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1586082Inhibition of human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID519600Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at trophozoites stage at 200 nM after 48 hrs by Giemsa staining based microscopy2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID417647Inhibition of human HDAC42009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID1853417Inhibition of human MMP-7 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID71648Inhibitory concentration against friend cells proliferation2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1862606Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1651336Selectivity ratio of IC50 for recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells to IC50 of human HDAC62020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID1862612Antiproliferative activity against human SK-OV-3 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID350024Increase in E-cadherin mRNA expression in human NCI-H661 cells at 300 nM by qRT-PCR relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.
AID1210091Increase in NAT1 enzyme activity in 40% confluent human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1605939Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID756005Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Dppa4 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID316876Inhibition of human SQ20B cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1387536Inhibition of human HDAC1 expressed in 293T cells at 100 uM using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay relative to control2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.
AID252223Average fold change in expression of CYP1A1 after treatment with compound of concentration 0.01 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID628434Inhibition of human recombinant HDAC5 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID519587Toxicity in neonatal foreskin fibroblasts2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID541647Inhibition of human HDAC8 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID360091Inhibition of TNF-alpha-induced tissue factor activity in HUVEC at 1 uM preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1901071Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as serum EPO level at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1833065Inhibition of recombinant C-terminal His-fusion tagged/N-terminal Strep2 tagged human HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID760387Inhibition of human recombinant HDAC4 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1656939Inhibition of mushroom tyrosinase using L-DOPA as substrate
AID366642Inhibition of HDAC3 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1702062Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins b2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1210099Induction of Sp1 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1246515Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1354370Antiproliferative activity against human MDA-MB-435 cells after 24 hrs by MTT assay
AID385448Inhibition of LPS-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of LPS challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1702061Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID242560Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 3b2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID1384760Inhibition of human HDAC2 using RHKKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID463864Inhibition of human HDAC in human HeLa cell nuclear extract at 50 nM after 15 mins by colorimetric assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.
AID1630587Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system using fluorogenic peptide RHKK(Ac) as substrate by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1246507Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1459972Inhibition of recombinant human HDAC8 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID313186Inhibition of HDAC4 expressed in 293T cells2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.
AID385455Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in p50 level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1605962Inhibition of HDAC10 (unknown origin) at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative to control2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1702064Inhibition of HDAC5 (unknown origin) using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID756010Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Oct3/4 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1605952Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1833063Inhibition of full length recombinant C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf21 insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence plate reader assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID420321Inhibition of Bordetella / Alcaligenes strain FB188 HDAC6 by fluorescence polarization assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID1280315Inhibition of human KDAC3 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID252221Average fold change in expression of CYP1B1 after treatment with compound of concentration 0.1 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID1578487Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID611685Inhibition of human HDAC6 using rhodamine as substrate after 1 hrs by fluorescence assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
AID90699Inhibitory activity against histone deacetylase (HDAC4) prepared from mouse melanoma B16/BL6 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
AID496802Inhibition of human HDAC22010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1586080Inhibition of human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1363781Inhibition of C-terminal His-tagged recombinant human HDAC8 expressed in baculovirus infected insect cells using RHKK(Ac)AMC as substrate by fluorescence-based assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery of the First-in-Class Dual Histone Deacetylase-Proteasome Inhibitor.
AID764214Inhibition of human recombinant HDAC1 using p53 residues 379-382 (RHKKAc) as substrate2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID90679Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells.2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1387552Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM measured immediately by immunoblot analysis2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.
AID252219Average fold change in expression of CYP1B1 after treatment with compound of concentration 1 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID1764792Inhibition of full length recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID760388Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1847753Antiproliferative activity against human T47D cells assessed as cell growth inhibition by burton method2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID1764793Selectivity index, ratio of IC50 for recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells to recombinant full length human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate pr2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID755998Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Otx2 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1479814Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus-infected Sf21 insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1709382Inhibition of recombinant human full-length C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 insect cells using RHKK(Ac)AMC as substrate preincubated for 5 to 10 mins followed by substrate addition and measured af2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID1622922Inhibition of recombinant full-length human HDAC7 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID308644Inhibition of human HDAC42007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID1882456Inhibition of HDAC1 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1702068Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1578485Inhibition of recombinant full length human HDAC1 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID708215Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.
AID659294Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2012European journal of medicinal chemistry, Jun, Volume: 52A novel series of l-2-benzyloxycarbonylamino-8-(2-pyridyl)-disulfidyloctanoic acid derivatives as histone deacetylase inhibitors: design, synthesis and molecular modeling study.
AID1246512Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID525002Inhibition of HDAC3 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1479819Inhibition of recombinant human HDAC10 expressed in baculovirus-infected insect cells using fluorogenic peptide RHKKAc as substrate by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID299642Inhibition of HDAC in HEK293 cells assessed as increase in histone H4 acetylation at 600 nM after 48 hrs relative to control2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition.
AID385471Effect on TNF-alpha-induced NF-kappaB activation assessed as p65/p50 binding to NF-kappaB in HUVEC at 1 uM preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID55804Cytotoxicity of compound against normal human prostate DU145 cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID233841Selectivity as ratio of inhibitory concentration for NFF cell line versus MM96L cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID385449Inhibition of TNF-alpha-induced tissue factor activity in C57BL/6J mouse macrophages preincubated for 4 hrs assessed after 5 hrs of TNFalpha challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID769928Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1847776Inhibition of HDAC4 in human HeLa cells incubated for 1 hr by mass spectrometry method2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID1591716Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID8302Compound was tested for antiproliferative activity against human A549 cancer cell lines using MTT assay2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID683277Antiproliferative activity against human BE(2)-C cells after 72 hrs by Alamar blue assay2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Amide-based derivatives of β-alanine hydroxamic acid as histone deacetylase inhibitors: attenuation of potency through resonance effects.
AID503116Induction of p27 expression in human HeLa cells at 1 uM after 24 hrs by Western blotting2007Nature chemical biology, Sep, Volume: 3, Issue:9
Spliceostatin A targets SF3b and inhibits both splicing and nuclear retention of pre-mRNA.
AID1635106Upregulation of HDAC1 inhibition/ERK signalling activation-mediated extracellular SOD protein expression in human THP1 cells at 1 uM after 24 hrs by ELISA2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells.
AID538409Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis2010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID90693Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID1622920Inhibition of recombinant full-length human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID90197Inhibitory concentration against histone deacetylase activity2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors.
AID1630621Inhibition of recombinant N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID769932Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID331899Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID1651332Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells by using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID516293Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH189 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1622973Inhibition of HDAC4 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID309970Induction of wild-type p21 promoter activation in mink Mv1Lu cells after 18 hrs by luciferase assay relative to basal level2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
AID1605955Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1254049Inhibition of HDAC8 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID385447Inhibition of IL-1-beta-induced tissue factor activity in human PBMC preincubated for 4 hrs assessed after 5 hrs of IL1-beta challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID417654Inhibition of human HDAC112009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID1322060Inhibition of human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using MOCPAC as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID324909Inhibition of human HDAC6 assessed as tubulin hyperacetylation in human HCT116 cells by Western blot2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).
AID516296Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH409 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID366643Inhibition of HDAC8 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID269912Inhibition of HDAC42006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID1182186Inhibition of human HDAC1 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID385467Induction of PMA-induced wild type NF-kappaB-dependent ICAM promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID760385Inhibition of human recombinant HDAC5 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1628748Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1127331Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1260647Inhibition of human recombinant HDAC11 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID104054Cytotoxicity of compound against normal human breast MCF-7 cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID541648Inhibition of human HDAC4 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1479812Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus-infected Sf9 insect cells using RHKK(Ac)AMC as substrate after 90 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1401561Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1177036Up-regulation of transcriptional activity of human CLA-1 promoter region -1055 to -62bp transfected in HepG2 cells by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID1431822Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID769927Induction of neurite outgrowth in rat PC12 cells at 10 uM after 5 days2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID309968Inhibition of human HDAC4 expressed in 293T cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
AID1605954Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to control2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID316887Antiproliferative activity against human MKN45 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID385451Reduction of ICAM1 mRNA level in TNF-alpha-stimulated HUVEC at 1 uM preincubated for 4 hrs assessed after 1 to 2 hrs of TNFalpha challenge by RT-PCR2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID503304Antiproliferative activity against human PC3 cells at 5 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID331900Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
AID1622924Inhibition of recombinant full-length human HDAC6 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1758519Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID525008Inhibition of HDAC7 in Fdelta508 CFTR-expressing human CFBE41o- cell line assessed as increase in cAMP-stimulated iodide efflux in at 0.1 uM after 24 hrs relative to control2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID309967Inhibition of human HDAC1 expressed in 293T cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
AID1532649Selectivity ratio of IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) to IC50 for recombinant C-terminal His-tagged human HDAC11 (1 to 347 residues)2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID1371055Inhibition of recombinant Trypanosoma brucei HDAC3 at 5 uM after 30 mins2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID90350Inhibitory activity against histone deacetylase (HDAC) enzyme obtained from H1299 human lung carcinoma cell lysates2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID1605940Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence 2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1479816Inhibition of recombinant human C-terminal GST-tagged HDAC4 expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1901145Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID240034Effective concentration determined for p21 promoter assay2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
AID1156700Cytotoxicity against human BGC823 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID1236442Inhibition of human HDAC12015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1647306Inhibition of human HDAC9 using fluorogenic Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence based analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID447994Inhibition of human recombinant HDAC3 after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID242587Inhibition concentration required to inhibit rat liver histone deacetylase (HDAC) in the presence of compound 5e as a substrate2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID209973Inhibition of acetylation of histone-4 in human T-24 cancer cells2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID240717Inhibition of human histone deacetylase 1 prepared from 293T cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
AID1260642Inhibition of human recombinant HDAC6 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID566555Inhibition of HDAC in human PC3 cells at 1 uM after 10 mins by fluorometric assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID478330Inhibition of HDAC in human HeLa cell nuclear extract assessed as inhibition of histone H4 deacetylation after 15 mins by fluorescence assay2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
Synthesis and biological activity of cyclotetrapeptide analogues of the natural HDAC inhibitor FR235222.
AID90671Inhibitory activity afgainst maize Histone deacetylase 1-A2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID299654Increase in GRP78 protein level in HEK293 cells at 600 nM by immunoblot2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition.
AID1647311Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorimetric assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1260643Inhibition of human recombinant HDAC7 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1765329Selectivity index, ratio of IC50 for human recombinant full length HDAC1 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1401626Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID568154Inhibition of HDAC6 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID1529534Antiproliferative activity against human BxPC3 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1586085Inhibition of human HDAC10 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID57526Cytotoxicity of compound against normal human melanoma DO4 cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1401601Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1702067Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1586077Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID417644Inhibition of human HDAC12009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID382112Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH reporter assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy.
AID1622990Antiproliferative activity against human A549 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1529533Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1622968Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1432955Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC62017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.
AID488358Inhibition of HDAC12010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
New orally bioavailable 2-aminobenzamide-type histone deacetylase inhibitor possessing a (2-hydroxyethyl)(4-(thiophen-2-yl)benzyl)amino group.
AID1431815Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID519584Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID385443Effect on TNF-alpha-induced IkappaB degradation in HUVEC at 1 uM preincubated for 4 hrs assessed after 60 mins of TNFalpha challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1127332Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1156704Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID385466Induction of PMA-induced TFkappaB mutant-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay relative to control2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID58061Inhibitory concentration required to reduce DU145 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID539709Inhibition of human HDAC after 30 mins2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.
AID385468Inhibition of LPS-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID652765Induction of CFTR deltaF508 mutant mRNA expression in cystic fibrosis patient lung cells relative to control2011ACS medicinal chemistry letters, Jul-21, Volume: 2, Issue:9
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of ΔF508-CFTR.
AID1518780Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID242559Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 3a2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID764211Selectivity ratio of IC50 for human recombinant HDAC1 to human recombinant HDAC62013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID385462Inhibition of LPS-induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of LPS challenge by luciferase reporter assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1401595Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1586084Inhibition of human HDAC9 using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID611683Inhibition of human HDAC1 using rhodamine as substrate after 1 hrs by fluorescence assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
AID541655Growth inhibition of human H460 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID367236Induction of histone H3 acetylation in human T24 cells2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID252225Average fold change in expression of CYP1B1 after treatment with compound of concentration 0.01 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID1647310Inhibition of recombinant human C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using Boc-K(Ac)-AMC as substrate after 60 mins by fluorimetry analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID525034In vivo inhibition of HDAC2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1647300Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1210095Increase in NAT1 mRNA expression in human HeLa cells at 0.5 uM after 24 hrs by qPCR method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1401605Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID73169Inhibitory concentration against normal fibroblast MRHF cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1155334Inhibition of Plasmodium falciparum recombinant histone deacetylase1 using HDAC substrate 3 as substrate at 1 uM by fluorescence assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID316886Antiproliferative activity against human SKBR3 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1479818Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus-infected insect cells after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID385454Reduction of tissue factor mRNA level in TNF-alpha-stimulated HUVEC at 1 uM preincubated for 4 hrs assessed after 1 to 2 hrs of TNFalpha challenge by RT-PCR2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1294953Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1384761Inhibition of human HDAC3 using RHKKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID106868Compound was tested for antiproliferative activity against human MKN45 cancer cell lines2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1401634Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1630624Inhibition of full length recombinant human HDAC11 expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID1881883Activation of PKM2 (unknown origin) Leu353, Glu397, Phe26, Gly315 residues2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
A Perspective on Medicinal Chemistry Approaches for Targeting Pyruvate Kinase M2.
AID764209Partition coefficient, log D of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID695598Inhibition of HDAC assessed as induction of p21 promoter expression by cell-based assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID541656Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID269915Selectivity for HDAC6 over HDAC42006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID769930Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1182188Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID1246516Inhibition of HDAC7 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID350025Increase in semaphoring 3F mRNA expression in human NCI-H661 cells at 300 nM by qRT-PCR relative to control2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.
AID538413Selectivity index, ratio of IC50 for recombinant human HDAC1 to IC50 for recombinant human HDAC62010Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23
Inhibitors selective for HDAC6 in enzymes and cells.
AID503527Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 9 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1390224Inhibition of recombinant mouse HDAC6 expressed in HEK293T cells co-expressing mouse HDA2 using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.
AID1246509Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID1557983Selectivity index, ratio of IC50 for recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate prei2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
AID769920Induction iof GAP-43 protein expression in rat PC12 cells after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID568152Inhibition of HDAC3 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID1431814Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC12017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1586079Inhibition of human HDAC3 using RHKKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1431816Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID1781509Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID1623248Inhibition of HDAC in HEK293 cells assessed as increase in histone H3 acetylation at Lys27 residues at 10 uM incubated for 24 hrs by Western blot analysis relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164The P-glycoprotein inhibitor diltiazem-like 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one inhibits esterase activity and H3 histone acetylation.
AID1431820Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC62017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID103356Inhibitory concentration required to reduce MCF-7 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID756021Inhibition of HDAC8 (unknown origin) after 30 mins by fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1518779Selectivity ratio of IC50 for human HDAC1 to IC50 for human HDAC62019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID1863439Inhibition of HDAC7 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1401627Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1173705Inhibition of HDAC1 (unknown origin) after 15 mins by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Aurones as histone deacetylase inhibitors: identification of key features.
AID723465Inhibition of human HDAC2 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1605953Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1155322Selectivity index, ratio of IC50 for erythrocytes (unknown origin) to IC50 for Plasmodium falciparum2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID764210Selectivity ratio of IC50 for human recombinant HDAC4 to human recombinant HDAC62013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID208533Concentration of compound required for acetylation of histone-4 in human T24 cancer cells2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Design and synthesis of a novel class of histone deacetylase inhibitors.
AID1781511Cytotoxicity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID708216Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.
AID1882462Inhibition of HDAC6 (unknown origin)2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology.
AID1155321Cytotoxicity against erythrocytes (unknown origin)2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1371070Antiparasitic activity against tachyzoite stage of Toxoplasma gondii2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1401592Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1 x 10'-5 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1556848Inhibition of HDAC8 (unknown origin) using R-H-K(Ac)-K(Ac)-AFC as substrate at 10 uM by fluorescence based assay2019European journal of medicinal chemistry, Oct-01, Volume: 179Selenocoumarins as new multitarget antiproliferative agents: Synthesis, biological evaluation and in silico calculations.
AID302799Inhibition of mouse recombinant HDAC6 expressed in 293 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
AID456800Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D62010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID1628756Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1401635Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID695594Inhibition of HDAC4 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID1401607Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1765328Inhibition of human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assa2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID620532Reactivation of MeCp2 mutant expression in human GM11272 cells at 1 to 100 nM by PCR method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression.
AID541645Inhibition of human HDAC2 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1354394Inhibition of HDAC8 (unknown origin) by ELISA
AID488276Inhibition of HDAC62010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1529531Antiproliferative activity against human U87 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1384766Selectivity index, ratio of IC50 for human HDAC3 to IC50 for human HDAC62018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID1628754Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1529529Antiproliferative activity against human K562R cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID621738Antiproliferative activity against human HCT116 cells by MTT assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors.
AID488274Inhibition of HDAC22010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1390227Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B-based colorimetric assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.
AID91803Cytotoxicity of compound against normal human ovarian JAM cell line2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine.
AID1236450Inhibition of human HDAC62015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1901147Inhibition of recombinant human full-length C-terminal Flag-His6-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID524995Inhibition of HDAC10 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1885254Inhibition of KDM4E (unknown origin)2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Recent Advances with KDM4 Inhibitors and Potential Applications.
AID1833069Selectivity ratio of IC50 for recombinant C-terminal His-fusion tagged/N-terminal Strep2 tagged human HDAC8 (1 to 377 residues) expressed in insect cells to IC50 full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected S2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID242600Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 12a2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID1390225Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B-based colorimetric assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.
AID1371053Antitrypanosomal activity against Trypanosoma brucei brucei measured after 22 hrs by fluorescence-based Alamar blue viability assay2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1401606Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1459974Inhibition of recombinant human HDAC10 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1236444Inhibition of human HDAC32015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1765325Inhibition of human full-length recombinant HDAC2 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID408883Inhibition of HDAC82008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID568156Inhibition of HDAC assessed as increase of histone H3 acetylation2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID316888Inhibition of HDAC from human SNU16 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID408881Inhibition of HDAC22008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1155340Inhibition of HDAC in Plasmodium falciparum 3D7 trophozoites assessed as histone H3 hyperacetylation level at 500 nM after 3 hrs by Western blotting analysis relative to control2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1901070Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma SCr concentration at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1862611Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1781508Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID269911Inhibition of HDAC12006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID1322066Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1578488Inhibition of recombinant full length human HDAC5 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1628762Antiproliferative activity against human MDA-MB-231 cells by WST8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1322067Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1210100Induction of Sp1 (GC>TA) mutant recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1156705Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID764208Intrinsic aqueous solubility of the compound at pH 7.4 by Avdeef-Tsinman potentiometric titration method2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).
AID331617Inhibition of human HDAC6 expressed in 293T cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
AID344918Inhibition of 2-oxoglutarate-dependent human JMJD2E preincubated for 30 mins by FDH coupled assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
AID1622993Antiproliferative activity against human SKBR3 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID525022Inhibition of HDAC in human CFBE41o- cell line assessed as increase in total CFTR protein level including CFTR glycoform at 0.1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1690113Selectivity index, ratio of IC50 for recombinant human HDAC8 to IC50 for recombinant human HDAC62020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID1622971Antiproliferative activity against human K562 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID414980Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID1384206Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1690111Selectivity index, ratio of IC50 for recombinant human C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 cells to IC50 for recombinant human HDAC62020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID1623249Inhibition of HDAC in human HepG2 cells assessed as increase in histone H3 acetylation at Lys27 residues at 10 uM incubated for 24 hrs by Western blot analysis relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164The P-glycoprotein inhibitor diltiazem-like 8-(4-chlorophenyl)-5-methyl-8-[(2Z)-pent-2-en-1-yloxy]-8H-[1,2,4]oxadiazolo[3,4-c][1,4]thiazin-3-one inhibits esterase activity and H3 histone acetylation.
AID81709Inhibitory concentration against human colon cancer HCT116 cell proliferation2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1895827Inhibition of HDAC6 (unknown origin)2021European journal of medicinal chemistry, Dec-15, Volume: 226Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020).
AID1591715Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay2019Bioorganic & medicinal chemistry, 08-01, Volume: 27, Issue:15
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.
AID1651333Inhibition of recombinant human C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID208400Inhibitory concentration required to reduce T24 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID90211Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Heterocyclic ketones as inhibitors of histone deacetylase.
AID90673Inhibitory activity against histone deacetylases (HDAC1) prepared from mouse melanoma B16/BL6 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
AID1853419Inhibition of human MMP-14 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID411793Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation.
AID1853414Inhibition of human MMP-1 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID1260637Inhibition of human recombinant HDAC1 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1605951Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1605945Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to 2 hrs by2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1173706Inhibition of HDAC2 (unknown origin) after 15 mins by fluorescence assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Aurones as histone deacetylase inhibitors: identification of key features.
AID1401623Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1605946Inhibition of HDAC9 (unknown origin) using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID302801Selectivity for human HDAC6 over human HDAC42007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
AID566558Inhibition of HDAC in human LNCAP cells at 1 uM after 10 mins by fluorometric assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
AID487227Inhibition of recombinant HDAC62010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID385439Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in p65 level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1210103Induction of acetylated histone H4 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by ChIP assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID769929Selectivity index, ratio of IC50 for human recombinant HDAC8 to IC50 for human recombinant HDAC62013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID102520Inhibitory concentration against lung A549 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1863440Inhibition of HDAC8 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1423498Inhibition of full length SIRT6 (unknown origin) using acetylated H3K9 peptide as substrate after 2 hrs in presence of NAD2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID316885Antiproliferative activity against human A549 cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID516283Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH754 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1156701Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID420329Inhibition of HDAC from RT extract2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Non-isotopic dual parameter competition assay suitable for high-throughput screening of histone deacetylases.
AID541650Inhibition of human HDAC7 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1847754Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID628432Inhibition of human recombinant HDAC7 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID568151Inhibition of HDAC2 by fluorescence assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID417653Inhibition of human HDAC102009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID331615Inhibition of human HDAC1 expressed in 293T cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
AID628437Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1578486Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID240719Inhibition of human histone deacetylase 6 prepared from 293T cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
AID241474Inhibitory concentration against maize histone deacetylase 22005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID1901067Antiproliferative activity against human HK-2 cells assessed as decrease in cell viability at 0.78 uM measured after 24 hrs by CCK-8 assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1394893Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC62018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID541649Inhibition of human HDAC5 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1862616Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1628747Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1394890Inhibition of human HDAC3 using RHKK(Ac) as substrate2018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1155320Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs2014European journal of medicinal chemistry, Jul-23, Volume: 82Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
AID1651335Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID1622967Inhibition of recombinant human HDAC4 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate measured after 30 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1765330Selectivity index, ratio of IC50 for human recombinant full length HDAC3 to IC50 for human recombinant full length HDAC22021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID324536Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 5.2 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID384317Inhibition of maize histone deacetylase 1A2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID516298Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate H0058-1-818 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID525030Inhibition of HDAC7 in human CFBE41o- cell line assessed as correction of mutant Fdelta508 CFTR trafficking to cell surface as glycoform at 0.1 uM by Immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1236445Inhibition of human HDAC82015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1280317Inhibition of human KDAC8 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1651334Inhibition of human HDAC6 using fluorogenic-(RHKKAc) as substrate by fluorescence assay2020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID81711Concentration required to inhibit the HCT116 cell growth by 50%.2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1432956Inhibition of human HDAC6 using RHKKAc as substrate by fluorescence assay2017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.
AID316881Inhibition of human MM96L cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1441632Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID503525Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 16 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID254794Inhibitory concentration against histone deacetylase 62005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Design and synthesis of phthalimide-type histone deacetylase inhibitors.
AID44724Inhibitory concentration against bladder T24 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID1479820Inhibition of recombinant human N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID417650Inhibition of human HDAC72009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID1280316Inhibition of human KDAC6 using [3H]acetyl histone H4 peptide substrate incubated for 60 mins by scintillation counting method2016Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.
AID1758521Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using [RHKK(Ac)] fluorogenic substrate2021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID723463Inhibition of human HDAC5 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID769931Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1371054Inhibition of recombinant Trypanosoma brucei HDAC1 at 5 uM after 30 mins2017Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives.
AID1702066Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC class2a as substrate measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1628749Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1605944Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID90515Effective concentration in histone deacetylases (HDAC) using p21 promoter assay2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
AID252220Average fold change in expression of CYP1A1 after treatment with compound of concentration 0.1 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID1503589Inhibition of HDAC in human HN13 cells assessed as reduction in histone H3 Lys9 acetylation incubated for 24 hrs by immunofluorescence assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Serendipitous discovery of potent human head and neck squamous cell carcinoma anti-cancer molecules: A fortunate failure of a rational molecular design.
AID80246Inhibitory activity against HCT116 human colon cell growth2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID384316Inhibition of maize histone deacetylase 1B2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID1586083Inhibition of human HDAC8 using RHKAcKAc as substrate by fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1690110Inhibition of recombinant human HDAC8 using RHK-K(Ac)-AMC as substrate by fluorescence based assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID385469Inhibition of TNF-alpha-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID302798Inhibition of human recombinant HDAC4 expressed in 293 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
AID506770Displacement of [3H]probe from SAP130 in human WiDr cell immunoprecipitate sample assessed as radioactive intensity at 500 nM after 1 hr by scintillation counting relative to control2007Nature chemical biology, Sep, Volume: 3, Issue:9
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
AID1605947Inhibition of HDAC10 (unknown origin) using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1635107Upregulation of HDAC1 inhibition/ERK signalling activation-mediated extracellular SOD mRNA expression in human THP1 cells at 1 uM after 24 hrs by RT-PCR method2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells.
AID90666Inhibitory activity on partially purified recombinant human Histone deacetylase 1 (HDAC-1)2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID461093Inhibition of HDAC62010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
AID503526Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 8 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1459969Inhibition of recombinant human HDAC4 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID70208Inhibitory concentration against normal epithelial HMEC cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID385461Effect on LPS-induced wild type NF-kappaB-dependent ICAM1 promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of LPS challenge by luciferase reporter assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID240720Inhibition of human histone deacetylase 8 prepared from 293T cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
AID506784Inhibition of SAP130 mediated cell growth in human WiDr cells2007Nature chemical biology, Sep, Volume: 3, Issue:9
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
AID1862620Inhibition of HDAC6 (unknown origin) measured by fluorometry assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID516299Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate H00581-1941 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID503694Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 12 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID447995Inhibition of human recombinant HDAC8 after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID254792Inhibitory concentration against histone deacetylase 22005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Design and synthesis of phthalimide-type histone deacetylase inhibitors.
AID1236446Inhibition of human HDAC42015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID299649Increase in protein disulfide isomerase level in HEK293 cells at 600 nM by immunoblot2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Induction of GRP78 by valproic acid is dependent upon histone deacetylase inhibition.
AID1622919Inhibition of recombinant full-length human HDAC8 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID465149Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1605957Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 h2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1273502Inhibition of HDAC in human HeLa cell nuclear extract using BML-KI104 Fluor de Lys as substrate by fluorescence-based assay2015Journal of natural products, Dec-24, Volume: 78, Issue:12
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.
AID541653Inhibition of human HDAC10 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1401628Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1294971Inhibition of human recombinant HDAC10 using RHK-K(Ac)-AMC as substrate2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID316891Inhibition of HDAC2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1210094Increase in NATa promoter activity in human HeLa cells at 0.5 uM after 24 hrs by qPCR method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID503682Inhibition of HDAC in human GM15850 cells assessed as increase in histone H3 lysine 14 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID541652Inhibition of human HDAC6 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1401639Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID90835Inhibitory activity against histone deacetylase 6 prepared from mouse melanoma B16/BL6 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
AID488273Inhibition of HDAC12010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID461095Inhibition of HDAC4 assessed as induction of p21 promotor activity by cell based assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
AID611686Inhibition of N terminal hexahistidine-tagged human HDAC8 expressed in Sf9 cells after 1 hr by fluorescence assay2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
AID1847752Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID367237Inhibition of human recombinant histone deacetylase 22009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID1401610Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.52 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID695592Inhibition of HDAC1 by fluorimetric assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.
AID360095Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID90208Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells.1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
Synthesis and histone deacetylase inhibitory activity of new benzamide derivatives.
AID755997Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Lhx1 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1853415Inhibition of human MMP-2 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID90675In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID1628752Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1532642Selectivity ratio of IC50 for human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) to IC50 for recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues)2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID78390Inhibitory concentration required to reduce H446 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID331618Induction of p21 expression in human HeLa cells after 24 hrs2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
AID1401594Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1622994Antiproliferative activity against human MKN45 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID516288Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B5788 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID90690In vitro for anti-HD2 (Histone deacetylase 2) activity in maize2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation.
AID269913Inhibition of HDAC62006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID1182187Inhibition of human HDAC4 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID302797Inhibition of human recombinant HDAC1 expressed in NIH3T3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
AID1628745Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID161227Inhibitory concentration against prostate DU145 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID525020Inhibition of HDAC in human CFBE41o- cell line assessed as total CFTR protein level including CFTR glycoform at 1 uM by immunoblot analysis2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID769924Induction of neurite outgrowth in human SH-SY5Y cells at 10 uM after 5 days2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID488275Inhibition of HDAC32010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
On the inhibition of histone deacetylase 8.
AID1656945Mixed-type of inhibition of mushroom tyrosinase using varying level of L-DOPA as substrate by Dixon plot analysis
AID274171Antiproliferative activity against HCT116 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID1401629Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID496808Activity of human HDAC82010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID465150Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID769914Inhibition of HDAC6 in rat PC12 cells assessed as acetylation of histone H3 at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID628433Inhibition of human recombinant HDAC6 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1210101Induction of Sp1 recruitment to NATb promoter in human HeLa cells nuclear extracts at 0.5 uM after 24 hrs by EMSA method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1622970Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1862614Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1690112Selectivity index, ratio of IC50 for recombinant human HDAC3 to IC50 for recombinant human HDAC62020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID760390Inhibition of human recombinant HDAC1 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID90521Inhibitory activity against histone deacetylase (HDAC)2003Bioorganic & medicinal chemistry letters, Jun-02, Volume: 13, Issue:11
Amide analogues of TSA: synthesis, binding mode analysis and HDAC inhibition.
AID1529526Inhibition of human recombinant HDAC11 after 30 mins using fluorogenic substrate by fluorimetric assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID670029Inhibition of HDAC1 in human MCF7 cells assessed as up-regulation of acetylated histone H3 protein level at 0.5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID90701Inhibition of Histone deacetylase 4 in mammalian cells2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1915533Agonist activity at Vitamin D receptor (unknown origin) by fluorescence polarization assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID417648Inhibition of human HDAC52009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID385463Inhibition of TNFalpha induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of TNFalpha challenge by luciferase reporter assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1628757Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID465153Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1424816Inhibition of human recombinant HDAC6 using RHKKAcAMC as substrate by fluorescence assay2018European journal of medicinal chemistry, May-25, Volume: 152Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors.
AID769916Inhibition of HDAC6 in rat PC12 cells assessed as induction of alpha-tubulin acetylation at 10 uM after 48 hrs by Western blotting analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1628753Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1324227Inhibition of HDAC2 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID1294969Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) expressed in insect cells/baculovirus expression system using RHK-K(Ac)-AMC as substrate by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1421931Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID525001Inhibition of HDAC2 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1833066Inhibition of full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 insect cells using RHK-K(Ac)-AMC as substrate measured after 90 mins by fluorescence plate reader assay2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID1605938Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by flu2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1690108Inhibition of recombinant human HDAC3 using RHK-K(Ac)-AMC as substrate by fluorescence based assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
AID385460Effect on TNF-alpha-induced wild type NF-kappaB-dependent ICAM1 promoter expression in HUVEC preincubated for 4 hrs assessed after 6 hrs of TNFalpha challenge by luciferase reporter assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1394895Selectivity index, ratio of IC50 for human HDAC8 to IC50 for human HDAC62018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1431819Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID600531Inhibition of HDAC in human HL60 cells assessed as increase in histone H3 acetylation at 20 ug/ml after 24 hrs by Western blot analysis2009Journal of natural products, Jul, Volume: 72, Issue:7
Cytotoxic triterpenoids from the stems of Microtropis japonica.
AID1529524Inhibition of human recombinant HDAC6 after 30 mins using fluorogenic substrate by fluorimetric assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID309969Inhibition of mouse HDAC6 expressed in 293T cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
AID1863441Inhibition of HDAC9 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1401638Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.37 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1254047Inhibition of HDAC1 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID723730Cytotoxicity against human A2780 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1532631Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID447993Inhibition of human recombinant HDAC1 after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID1479813Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in baculovirus-infected insect cells using RHK(Ac)K(Ac)AMC as substrate after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1322068Selectivity index, ratio of IC50 for HDAC1 in human SHSY5Y cells to IC50 for HDAC6 in human SHSY5Y cells2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1441630Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID273990Inhibition of HDAC12007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.
AID1384764Selectivity index, ratio of IC50 for human HDAC1 to IC50 for human HDAC62018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID302800Selectivity for human HDAC6 over human HDAC12007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.
AID1432957Inhibition of human HDAC1 using RHKKAc as substrate by fluorescence assay2017ACS medicinal chemistry letters, May-11, Volume: 8, Issue:5
Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.
AID1862610Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1863442Inhibition of HDAC10 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1446915Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy.
AID324910Inhibition of human HDAC1 assessed as histone hyperacetylation in human HCT116 cells by Western blot2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).
AID252218Average fold change in expression of CYP1A1 after treatment with compound of concentration 1 mM in human MCF-7 cells2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Effects of suberoylanilide hydroxamic acid and trichostatin A on induction of cytochrome P450 enzymes and benzo[a]pyrene DNA adduct formation in human cells.
AID254791Inhibitory concentration against histone deacetylase 12005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Design and synthesis of phthalimide-type histone deacetylase inhibitors.
AID1635111Inhibition of HDAC1 in human THP1 cells assessed as increase in histone H3 acetylation level at 1 uM after 12 hrs by Western blot analysis relative to control2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells.
AID496805Inhibition of human HDAC52010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1266100Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1401611Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1354391Inhibition of human HDAC1 by ELISA
AID1656942Cytotoxicity against human A549 cells assessed as reduction in cell viability
AID90528Inhibition of histone deacetylase (HDAC) activity in HeLa cell nuclear extract2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides.
AID769935Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1758523Selectivity ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62021European journal of medicinal chemistry, May-05, Volume: 217Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.
AID360097Inhibition of HOSCN-induced tissue factor protein expression in HUVEC preincubated for 4 hrs assessed after 4 hrs of HOSCN challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID90359Concentration required for inhibition of histone deacetylase HD2 in vitro.2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity.
AID269914Selectivity for HDAC6 over HDAC12006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate.
AID496803Inhibition of human HDAC32010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID456798Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID756007Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Rex1 expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID1605941Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID385464Induction of PMA-induced wild type TFkappaB-dependent tissue factor promoter expression in HUVEC at 100 nM preincubated for 4 hrs assessed after 6 hrs of PMA challenge by luciferase reporter assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID90351Concentration required to inhibit human Histone deacetylase (HDAC) enzyme by 50%2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1529525Inhibition of human recombinant HDAC8 after 30 mins using fluorogenic substrate by fluorimetric assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID408880Inhibition of HDAC12008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID408884Inhibition of HDAC102008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum.
AID1276711Inhibition of recombinant human HDAC1 by fluorimetry2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.
AID1630619Inhibition of recombinant C-terminal His-tagged/N-terminal GST-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID456797Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID628430Inhibition of human recombinant HDAC10 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1853422Inhibition of human HDAC8 at 0.5 uM by fluorometric method2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID503693Inhibition of HDAC in human GM15850 cells assessed as increase in histone H4 lysine 5 acetylation of FXN gene at 0.1 uM after 96 hrs by chromatin immunoprecipitation assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID90522Inhibitory concentration against rat liver Histone deacetylase2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID516291Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B3939 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1324228Inhibition of HDAC3 (unknown origin) assessed as inhibition of fluorogenic peptide deacetylation2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.
AID90687Inhibitory concentration against maize Histone deacetylase 22003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID273167Inhibition of maize HD1A2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID242687Inhibitory concentration against human histone deacetylase (HDAC) from HeLa cells with substrate 5a2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID313187Inhibition of HDAC6 expressed in 293T cells2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.
AID756022Inhibition of HDAC1 (unknown origin) after 30 mins by fluorometric analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID385442Increase in acetylated histone H3 level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blot2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1236448Inhibition of human HDAC72015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID760389Inhibition of human recombinant HDAC2 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID1294965Inhibition of human recombinant N-terminal GST-tagged C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID302099Antiproliferative activity against H661 cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Antiproliferative activities of a library of hybrids between indanones and HDAC inhibitor SAHA and MS-275 analogues.
AID1833067Selectivity ratio of IC50 for full length recombinant C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf21 insect cells to IC50 for full length recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 in2021Bioorganic & medicinal chemistry, 11-15, Volume: 50Effect of phenylurea hydroxamic acids on histone deacetylase and VEGFR-2.
AID1210102Induction of Sp1 recruitment to NATb promoter in human HeLa cells at 0.5 uM after 24 hrs by ChIP assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID525003Inhibition of HDAC1 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID80076Inhibitory activity against H1299 human lung carcinoma cell growth2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824).
AID308645Inhibition of human HDAC62007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
AID90688Inhibitory activity against maize Histone deacetylase 2 at 1 mM2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID358670Induction of REST/NRSF-coupled repression of luciferase tagged rat RE1/NRSE BDNF promoter activity expressed in ST14A cells assessed as increase in luciferase activity2007The Journal of biological chemistry, Aug-24, Volume: 282, Issue:34
Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators.
AID243634In vitro inhibition against human Histone deacetylase2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors.
AID1254048Inhibition of HDAC6 (unknown origin) incubated for 1 hr by fluor de lys substrate based fluorescence method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.
AID1127325Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1322065Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1182189Ratio of IC50 for mouse HDAC6 to IC50 for human HDAC12014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
AID650228Inhibition of HDAC22012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain.
AID1431821Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC82017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID90696Inhibition of maize histone deacetylase 22004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 3. Discovery of novel lead compounds through structure-based drug design and docking studies.
AID417652Inhibition of human HDAC92009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
AID1322062Selectivity index, ratio of IC50 for human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells to IC50 for human recombinant HDAC6 expressed in baculovirus infected insect cells2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1401599Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1156699Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID541651Inhibition of human HDAC9 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID516285Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH535 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID500916Inhibition of heat-induced AML1-ETO protein expression in heterozygous transgenic zebrafish embryo at 0.5 uM by Western blot analysis2009Nature chemical biology, Apr, Volume: 5, Issue:4
Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation.
AID1530556Inhibition of recombinant human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by homogeneous fluorescence release assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Identification of novel quinazoline derivatives as potent antiplasmodial agents.
AID1630620Inhibition of recombinant C-terminal His-tagged human HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus expression system using fluorogenic substrate at 100 uM by fluorescence assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of santacruzamate A analogues for anti-proliferative and immunomodulatory activity.
AID447991Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID309971Selectivity for human HDAC4 over human HDAC12007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework.
AID1423499Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins by fluorescence-based SDS-denaturation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID1293871Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 200 nM after 24 hrs by fluorescence microscopy2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID525000Inhibition of HDAC4 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID708214Selectivity index, ratio of IC50 for human recombinant HDAC1 to IC50 for human recombinant HDAC62012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.
AID605940Antifungal activity against Saccharomyces cerevisiae ATCC 9763 by microdilution method2011Journal of natural products, May-27, Volume: 74, Issue:5
Microbial transformation of trichostatin A to 2,3-dihydrotrichostatin A.
AID367240Selectivity ratio of IC50 for human recombinant histone deacetylase 2 to IC50 for human recombinant histone deacetylase 62009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID414981Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
AID524994Inhibition of HDAC9 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID242561Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 5a2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID1401631Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1529564Antiproliferative activity against human HT-29 cells in presence of isoCA-4 after 72 hrs by MTS assay relative to control2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1294968Inhibition of human recombinant C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID360092Inhibition of IL-1-beta-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of IL1-beta challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1622969Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID775831Inhibition of HDAC2 (unknown origin)-mediated deacetylation at 10 uM preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Investigating the selectivity of metalloenzyme inhibitors.
AID274170Antiproliferative activity against H1299 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID201624Compound was tested for antiproliferative activity against human SK-BR-3 cancer cell lines2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1622972Inhibition of HDAC1 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID519602Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at schizonts stage at 200 nM after 48 hrs by Giemsa staining based microscopy2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1659230Inhibition of human HDAC12020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
AID723479Inhibition of HDAC in cisplatin resistant human A2780 cells after 18 hrs by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID385456Effect on TNF-alpha-induced SP1 protein level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1294963Inhibition of full length human recombinant C-terminal GST-tagged HDAC2 (1 to 488 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID755481Inhibition of recombinant human HDAC1 using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID1651338Selectivity ratio of IC50 for recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells to IC50 of human HDAC62020Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3
Synthesis and biological evaluation of 2-quinolineacrylamides.
AID1635110Inhibition of HDAC1 in human THP1 cells assessed as increase in histone H4 acetylation level at 1 uM after 12 hrs by Western blot analysis relative to control2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Royal Jelly Constituents Increase the Expression of Extracellular Superoxide Dismutase through Histone Acetylation in Monocytic THP-1 Cells.
AID463865Inhibition of human HDAC in human HeLa cell nuclear extract after 15 mins by colorimetric assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
SelSA, selenium analogs of SAHA as potent histone deacetylase inhibitors.
AID80247Inhibitory concentration required to reduce HCT 116 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID1622917Inhibition of recombinant full-length human HDAC2 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID273173Inhibition of mouse HDAC12006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1605943Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID628436Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
AID1530557Inhibition of recombinant human HDAC6 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Identification of novel quinazoline derivatives as potent antiplasmodial agents.
AID1246517Inhibition of HDAC9 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID226263Fold selectivity for classI HDAC2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1652187Inhibition of human recombinant HDAC1 using fluorogenic substrate incubated for 30 mins by fluorescence based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.
AID1863435Inhibition of HDAC3 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1595396Inhibition of HDAC in human HeLa nuclear extract assessed as enzyme residual activity at 5 nM using Boc-Lys(acetyl)-AMC as substrate and measured after 15 mins by fluorescence assay relative to control2019European journal of medicinal chemistry, Jun-15, Volume: 172Targeting gliomas with triazene-based hybrids: Structure-activity relationship, mechanistic study and stability.
AID1459968Inhibition of recombinant human HDAC3 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID516297Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH771 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID239792Selectivity for class I HDACs as ratio of IC50 for maize histone deacetylase 1-A and 1-B2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID43462Inhibitory concentration against breast MDA-MB-231 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID496809Inhibition of human HDAC92010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID456801Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W22010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group.
AID516289Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B5763 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1246514Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID524822Inhibition of HDAC7 in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 0.1 uM2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID760386Inhibition of human recombinant HDAC6 by Michaelis-Menten equation analysis2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
AID366641Inhibition of HDAC2 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1518781Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.
AID367235Induction of alpha tubulin acetylation in human T24 cells2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID525035Inhibition of CFTR transcription assessed as decrease of CFTR protein level at 50 uM by immunoblot method2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID1454738Decrease in alcohol intake in rat assessed as ethanol intake at 2 mg/kg, ip administered daily during last 3 days of 10 day period of two-bottel choice paradigm (Rvb = 7 g/kg)2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Class I HDAC Inhibitors: Potential New Epigenetic Therapeutics for Alcohol Use Disorder (AUD).
AID1765327Inhibition of human full-length recombinant HDAC6 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay2021European journal of medicinal chemistry, Oct-15, Volume: 222A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles.
AID1473143Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorescence assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
(N-Hydroxycarbonylbenylamino)quinolines as Selective Histone Deacetylase 6 Inhibitors Suppress Growth of Multiple Myeloma in Vitro and in Vivo.
AID385458Inhibition of TNF-alpha-induced p65 binding to TFkappaB in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID71776Tested in vivo for the inhibition of proliferation of friend leukemic cells2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID350022Inhibition of HDAC in human NCI-H661 cells assessed as induction of alpha-tubulin acetylation at 300 nM after 6 hrs by Western blot analysis2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.
AID1431812Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC32017European journal of medicinal chemistry, Feb-15, Volume: 127Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors.
AID242586Inhibitory concentration against rat liver histone deacetylase (HDAC) with substrate 5b2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Subtype selective substrates for histone deacetylases.
AID83150Inhibitory concentration required to reduce normal human epithelial cell line (HMEC), growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID755478Inhibition of recombinant human HDAC4 using acetyl-Lys-(trifluoroacetyl)-AMC as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID1702069Inhibition of N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID1605960Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence as2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1605961Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1293876Inhibition of HDAC in human HeLa nuclear extract assessed as accumulation of acetylated histone H3 after 24 hrs by western blot analysis2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.
AID1901069Nephroprotective activity against cisplatin-induced acute kidney injury in male C57BL/6 mouse assessed as plasma BUN concentration at 10 mg/kg/day, ip2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID1532639Inhibition of recombinant C-terminal His-tagged human HDAC11 (1 to 347 residues) expressed in Baculovirus infected insect cells using RHKK-Ac as substrate by fluorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID1589336Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Design, synthesis and biological evaluation of novel isoindolinone derivatives as potent histone deacetylase inhibitors.
AID1260646Inhibition of human recombinant HDAC10 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID1401596Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.23 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID524997Inhibition of HDAC7 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID313185Inhibition of HDAC1 expressed in 293T cells2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Interaction of aliphatic cap group in inhibition of histone deacetylases by cyclic tetrapeptides.
AID1628755Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1276713Inhibition of recombinant human HDAC8 by fluorimetry2016Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.
AID519709Antimalarial activity against Plasmodium falciparum infected in O+ human erythrocytes assessed as reduction in parasites at ring stage at 200 nM after 48 hrs by Giemsa staining based microscopy2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1354393Inhibition of HDAC3 (unknown origin) by ELISA
AID1401558Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID608776Inhibition of HDAC in human HeLa cells using Ac-Arg-Gly-Lys(Ac)-AMC as fluorescent substrate after 20 mins by fluorescence assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure-based optimization of click-based histone deacetylase inhibitors.
AID50591Inhibitory concentration against colon SW48 cell line2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
AID274375Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin by Western blot analysis at 0.1 uM2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.
AID1578489Inhibition of recombinant full length human HDAC7 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
AID1605949Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID516294Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate NIH34 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1628761Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1656943Cytotoxicity against human MCF7 cells assessed as reduction in cell viability
AID1702060Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay2018Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
AID461091Inhibition of HDAC12010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Bicyclic peptides as potent inhibitors of histone deacetylases: optimization of alkyl loop length.
AID1901052Inhibition of HDAC in human HK-2 cells assessed as increase in histone H3 expression acetylation at 5 uM measured by western blot analysis2022European journal of medicinal chemistry, Feb-15, Volume: 230Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
AID274169Antiproliferative activity against H661 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of rigid trichostatin A analogs as HDAC inhibitors.
AID1394894Selectivity index, ratio of IC50 for human HDAC3 to IC50 for human HDAC62018European journal of medicinal chemistry, Apr-25, Volume: 1501-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.
AID1401603Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.33 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID90668Inhibitory concentration against recombinant human Histone deacetylase 12003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID1210096Effect on NAT1 mRNA stability in human HeLa cells assessed as slope of mRNA decay curve at 0.5 uM after 24 hrs in presence of transcription inhibitor actinomycin D by qPCR method (Rvb = -0.78 +/- 0.02/hr)2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1401641Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 5.08 x 10'-10 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID756009Inhibition of HDAC8 in C57BL/6 mouse embryonic fibroblasts assessed as upregulation of Nanog expression after 24 hrs by qPCR analysis2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity.
AID90682Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells.
AID487225Inhibition of recombinant HDAC22010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID1622926Inhibition of recombinant full-length human HDAC11 using RHKK(Ac) as substrate measured after 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158HDAC as onco target: Reviewing the synthetic approaches with SAR study of their inhibitors.
AID1628758Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID1210098Induction of NATb Sp1 site in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID516282Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH200 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1529527Antiproliferative activity against human A549 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID316880Inhibition of mouse liver HDAC12008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID465151Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID1529530Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID385453Decrease in thioglycolate-induced tissue factor activity in C57BL/6J mouse macrophage at 1 mg/kg, ip preincubated for 4 hrs assessed after 5 hrs of thioglycolate challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID367239Inhibition of human recombinant histone deacetylase 82009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID516290Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH198 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1421930Antiplasmodial activity against Plasmodium falciparum2018European journal of medicinal chemistry, Oct-05, Volume: 158One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
AID350021Inhibition of HDAC in human NCI-H661 cells assessed as induction of histone H4 acetylation at 300 nM after 6 hrs by Western blot analysis2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.
AID1210097Induction of NATb 3657 bp fragment upstream of exon 4 in human HeLa cells at 0.5 uM after 24 hrs by luciferase reporter gene assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID1423500Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of ADP-ribose by fluorescence-based SDS-denaturation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID1647301Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminaL GST-tagged human recombinant NCOR2 (395 to 489 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 60 mins b2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1246511Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID769934Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Quinazolin-4-one derivatives as selective histone deacetylase-6 inhibitors for the treatment of Alzheimer's disease.
AID1384763Inhibition of human HDAC6 using RHKKAc peptide as substrate2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID385457Effect on TNF-alpha-induced Egr1 protein level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blotting2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID286454Inhibition of Histone deacetylase in HeLa cell nuclear extracts by fluorescence-based assay2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Design and synthesis of a potent histone deacetylase inhibitor.
AID366645Inhibition of HDAC10 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID1260644Inhibition of human recombinant HDAC8 at 20 uM using Ac-RHK(Ac)K(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID382342Inhibition of human HDAC in HeLa cells by flour de lys assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
AID503668Cytotoxicity against human GM15850 cells at 5 uM after 96 hrs by trypan blue exclusion assay2006Nature chemical biology, Oct, Volume: 2, Issue:10
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
AID1236449Inhibition of human HDAC92015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID506769Displacement of [3H]probe from SAP130 in human WiDr cells assessed as radioactive intensity at 500 nM after 1 hr by scintillation counting relative to control2007Nature chemical biology, Sep, Volume: 3, Issue:9
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
AID331616Inhibition of human HDAC4 expressed in 293T cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
AID240718Inhibition of human histone deacetylase 4 prepared from 293T cells2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.
AID385441Increase in acetylated histone H4 level in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by Western blot2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID90672Inhibitory activity against maize Histone deacetylase 1-B2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Discovery of (aryloxopropenyl)pyrrolyl hydroxyamides as selective inhibitors of class IIa histone deacetylase homologue HD1-A.
AID1528345Inhibition of human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHKKAc as substrate2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.
AID541654Inhibition of human HDAC11 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID541644Inhibition of human HDAC1 by fluorimetric assay2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity.
AID1628759Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay2016Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
AID519604Inhibition of HDAC in Plasmodium falciparum Dd2 infected in O+ human erythrocytes assessed as alteration of histone acetylation at 500 nM after 3.5 hrs by Westen blot2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID241538Inhibitory concentration against maize histone deacetylase 1-B (class I HDAC)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID1294964Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID1529562Antiproliferative activity against human HT-29 cells assessed as cell viability after 72 hrs by MTS assay relative to control2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4.
AID1210090Increase in NAT1 enzyme activity in human HeLa cells at 0.5 uM using p-aminobenzoic acid substrate after 24 hrs by HPLC method relative to untreated control2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID273166Inhibition of maize HD22006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Synthesis and biological properties of novel, uracil-containing histone deacetylase inhibitors.
AID1781510Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by EZ-Cytox colorimetric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID1387553Inhibition of HDAC in human HeLaS3 cells assessed as increase in histone H3K9 acetylation at 10 uM treated for 16 hrs followed by compound washout and measured up to 24 hrs by immunoblot analysis2018ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9
Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.
AID487224Inhibition of recombinant HDAC12010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID723461Inhibition of human HDAC8 by fluorescence assay2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against chemoresistant cancer cells.
AID1441631Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID1401625Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 3.70 x 10'-7 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID516287Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate B4506 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1525777Inhibition of HADC1 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1459953Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID1322059Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa nuclear extracts using MAL as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Synthesis of a selective HDAC6 inhibitor active in neuroblasts.
AID1401604Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1647309Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorimetry analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.
AID1294966Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID385440Effect on TNF-alpha-induced NF-kappaB activation in HUVEC preincubated for 4 hrs assessed as increase in c-Rel level after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1294961Inhibition of HDAC1 in human HeLa cells assessed as hyperacetylation of histone H3 at 2 uM incubated for 24 hrs by Western blot analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Computer-aided identification of new histone deacetylase 6 selective inhibitor with anti-sepsis activity.
AID385459Inhibition of TNF-alpha-induced p65 binding to ICAM1 NF-kappaB in HUVEC preincubated for 4 hrs assessed after 0.5 hrs of TNFalpha challenge by chromatin immunoprecipitation assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID544397Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation at 100 nM after 3.5 hrs by SDS-PAGE2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.
AID1246513Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
AID496801Inhibition of human HDAC12010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID465152Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents.
AID519583Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Potent antimalarial activity of histone deacetylase inhibitor analogues.
AID1764798Inhibition of class1 HDAC in mouse Neuro2a cells assessed as fold increase in ratio of acetylated histone H3 to histone H4 at 1 uM incubated for overnight by Western blot analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
AID1156702Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID385444Effect on TNF-alpha-induced TFkappaB activation assessed as p65/c-Rel binding to TFkappaB in HUVEC preincubated for 4 hrs measured after 0.5 hrs of TNFalpha challenge by electrophoretic shift mobility assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID1401637Inhibition of HDAC10 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.06 to 107.72%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1532629Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate by fluorimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Highly fluorescent and HDAC6 selective scriptaid analogues.
AID201882Inhibitory concentration required to reduce SW48 tumor cell growth by 50% in MTT assay2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
AID1605958Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative t2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1441699Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins2017Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5
Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis.
AID568157Inhibition of HDAC assessed as increase of histone H4 acetylation2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Structure and property based design, synthesis and biological evaluation of γ-lactam based HDAC inhibitors.
AID1390223Inhibition of recombinant human HDAC1 expressed in HEK293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins in presence of DTT by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and biological evaluation of histone deacetylase and DNA topoisomerase II-Targeted inhibitors.
AID1862622Inhibition of HDAC11 (unknown origin) measured by fluorometry assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID80362In vitro antiproliferative activity against human colon cancer HCT 116 cells determined by MMT assay2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Design and synthesis of a novel class of histone deacetylase inhibitors.
AID1659237Inhibition of human HDAC6 (unknown origin)2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.
AID1853416Inhibition of human MMP-3 at 0.5 uM2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID1384768Selectivity index, ratio of IC50 for human HDAC10 to IC50 for human HDAC62018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer's Disease Phenotypes.
AID1177037Cytotoxicity against human U2OS cells after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID1236447Inhibition of human HDAC52015Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
AID1459975Inhibition of recombinant human HDAC11 using fluorogenic substrate by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 1253-Aroylindoles display antitumor activity in vitro and in vivo: Effects of N1-substituents on biological activity.
AID90349Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.
AID1177039Cytotoxicity against human HeLa cells after 96 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909.
AID90344Induction of p21 using Histone deacetylase inhibitors2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
AID1210093Increase in NATb promoter activity in human HeLa cells at 0.5 uM after 24 hrs by qPCR method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Histone deacetylase inhibitors increase human arylamine N-acetyltransferase-1 expression in human tumor cells.
AID316883Selectivity index, ratio of IC50 for human MM96L cells to IC50 for human NFF cells2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Histone deacetylase inhibitors: from bench to clinic.
AID1781513Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate incubated for 20 mins by fluorometric assay2021Journal of natural products, 09-24, Volume: 84, Issue:9
Ulleunganilines A-C, Trichostatin Analogues Bearing a Modified Side Chain from
AID1401624Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 1.11 x 10'-6 M after 1 to 2 hrs by fluorescence assay (Rvb = 96.3 to 101.70%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID621737Inhibition of HDAC1 by fluorescent activity assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors.
AID1127329Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate2014European journal of medicinal chemistry, May-22, Volume: 79Influence of the adamantyl moiety on the activity of biphenylacrylohydroxamic acid-based HDAC inhibitors.
AID1853421Inhibition of human HDAC3 at 0.5 uM by fluorometric method2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
AID1525776Inhibition of HADC6 (unknown origin)2020Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.
AID1605956Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.
AID1479815Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged recombinant human NCOR2 (395 to 489 residues) expressed in baculovirus-infected insect cells using RHKK(Ac)AMC as substrate after 60 mins by fluorimeter2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors.
AID1901146Inhibition of C-terminal His-tagged human HDAC3 (1 to 428 residues)/N-terminal GST tagged human NCOR2 (395 to 489) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC substrate measured after 30 mins by fluorimetry2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.
AID360093Inhibition of HOSCN-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of HOSCN challenge by one stage clotting assay2007The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
Histone deacetylase inhibitors suppress TF-kappaB-dependent agonist-driven tissue factor expression in endothelial cells and monocytes.
AID755475Inhibition of recombinant human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID500920Inhibition of Hsp70 expression in heterozygous transgenic zebrafish embryo at 0.5 uM by Western blot analysis2009Nature chemical biology, Apr, Volume: 5, Issue:4
Discovering chemical modifiers of oncogene-regulated hematopoietic differentiation.
AID366640Inhibition of HDAC1 after 17 hrs2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
AID516292Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype B isolate NIH184 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1863436Inhibition of HDAC4 (unknown origin) by colorimetric method2022European journal of medicinal chemistry, Oct-05, Volume: 240Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier.
AID1423501Binding affinity to recombinant human full length SIRT6 (1 to 355 residues) expressed in Escherichia coli M15 after 20 mins in presence of ADP-ribose and acetylated H3K9 peptide by fluorescence-based SDS-denaturation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID1156706Cytotoxicity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents.
AID1423503Inhibition of human SIRT6 preincubated for 5 mins in presence of substrate followed enzyme addition measured after 5 to 10 mins in presence of NAD by fluorescence spectrophotometry2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development.
AID1709384Selectivity index, ratio of IC50 for inhibition of recombinant human full-length C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf9 insect cells to IC50 for inhibition of recombinant human full-length N-terminal GST2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.
AID90519Inhibitory concentration against partially purified mouse histone deacetylase (HDAC)2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Histone deacetylase inhibitors.
AID421211Antitumor activity against mouse ML1 cells2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Recent advances in the development of polyamine analogues as antitumor agents.
AID1401597Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.12 x 10'-8 M after 1 to 2 hrs by fluorescence assay (Rvb = 93.78 to 100%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID755479Inhibition of HDAC3/NCOR2 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate assessed as residual activity at 3.3 x 10'-5 M after 2 hrs by fluorescence assay relative to control2013Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
Structural basis for the design and synthesis of selective HDAC inhibitors.
AID1266099Inhibition of HDAC6 in human HeLa cells assessed as tubulin acetylation incubated for overnight by immunofluorescence microscopic analysis2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
AID1260645Inhibition of human recombinant HDAC9 at 20 uM using Boc-Lys(Tfa)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID384318Selectivity for IC50 of maize histone deacetylase 1B over IC50 of maize histone deacetylase 1A2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Class II-selective histone deacetylase inhibitors. Part 2: alignment-independent GRIND 3-D QSAR, homology and docking studies.
AID367238Inhibition of human recombinant histone deacetylase 62009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
AID496780Inhibition of shATP citrate lyase-induced cell differentiation in mouse C2C12 assessed as myosin heavy chain expression at 100 nM2010Nature chemical biology, Mar, Volume: 6, Issue:3
Carbon metabolism-mediated myogenic differentiation.
AID1401609Inhibition of HDAC2 (unknown origin) using RHKK(Ac)AMC as substrate assessed as remaining activity at 4.57 x 10'-9 M after 1 to 2 hrs by fluorescence assay (Rvb = 94.78 to 103.8%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID241537Inhibitory concentration against maize histone deacetylase 1-A (class IIa HDAC)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides.
AID516286Antimicrobial activity against fluconazole-resistant Cryptococcus gattii serotype C isolate NIH257 at 64 ug/ml2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Heteroresistance of Cryptococcus gattii to fluconazole.
AID1862609Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1845905Reversal of HIV-1 latency infected in human J-Lat Tat-GFP Clone A7 cells assessed as increase in GFP expressing cells at 100 nM incubated for 72 hrs by flow cytometry analysis relative to control2021European journal of medicinal chemistry, Mar-05, Volume: 213HIV latency reversal agents: A potential path for functional cure?
AID670035Inhibition of HDAC6 in human MCF7 cells assessed as change in tubulin acetylation level at 0.5 uM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Defining the mechanism of action and enzymatic selectivity of psammaplin A against its epigenetic targets.
AID1401560Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate after 1 to 2 hrs by fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors.
AID1202473Antiproliferative activity against human A549 cells assessed as shrunken and sharp shape at 0.4 uM after 24 hrs by phase contrast microscopy2015European journal of medicinal chemistry, , Volume: 96Efficient synthesis and biological activity of Psammaplin A and its analogues as antitumor agents.
AID1354392Inhibition of human HDAC2 by ELISA
AID1530555Inhibition of recombinant human HDAC1 using RHK-K(Ac) as substrate by homogeneous fluorescence release assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Identification of novel quinazoline derivatives as potent antiplasmodial agents.
AID1260639Inhibition of human recombinant HDAC3 at 20 uM using Boc-Lys(Ac)-AMC as substrate after 30 to 60 mins by microplate reader assay
AID447992Inhibition of HDAC in human HeLa cell cytosolic extract after 30 mins by fluorimetric assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
AID524998Inhibition of HDAC5 by in vitro deacetylation assay2010Nature chemical biology, Jan, Volume: 6, Issue:1
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
AID496804Inhibition of human HDAC42010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1802398Enzymatic HDAC Activity Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1802451HDAC Cell-Free Assays from Article 10.1074/jbc.M113.472563: \\The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.\\2013The Journal of biological chemistry, Nov-22, Volume: 288, Issue:47
The antiparasitic clioquinol induces apoptosis in leukemia and myeloma cells by inhibiting histone deacetylase activity.
AID1802399Proteros Reporter Displacement Assay from Article 10.1074/jbc.M113.490706: \\Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.\\2013The Journal of biological chemistry, Sep-13, Volume: 288, Issue:37
Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2008The Journal of biological chemistry, Apr-25, Volume: 283, Issue:17
Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1346090Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346032Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346066Human histone deacetylase 5 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346134Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346104Human histone deacetylase 4 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346131Human histone deacetylase 7 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346068Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346077Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID1346082Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs))2010Nature chemical biology, Mar, Volume: 6, Issue:3
Chemical phylogenetics of histone deacetylases.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Inside HDAC with HDAC inhibitors.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB1999Nature, Sep-09, Volume: 401, Issue:6749
Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors.
AID1811Experimentally measured binding affinity data derived from PDB1999Nature, Sep-09, Volume: 401, Issue:6749
Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,311)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (0.15)18.7374
1990's147 (4.44)18.2507
2000's1563 (47.21)29.6817
2010's1424 (43.01)24.3611
2020's172 (5.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 112.76

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index112.76 (24.57)
Research Supply Index8.12 (2.92)
Research Growth Index6.72 (4.65)
Search Engine Demand Index206.94 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (112.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (0.21%)5.53%
Reviews57 (1.69%)6.00%
Case Studies4 (0.12%)4.05%
Observational1 (0.03%)0.25%
Other3,296 (97.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Tolerability Study of Trichostatin A In Subjects With Relapsed or Refractory Hematologic Malignancies [NCT03838926]Phase 142 participants (Anticipated)Interventional2018-09-27Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]