Page last updated: 2024-11-08

pifithrin mu

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Description

2-phenylacetylenesulfonamide: induces p53-independent apoptotic killing of B-chronic lymphocytic leukemia cells; also inhibits Hsp70 and autophagy [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID327653
CHEMBL ID1241268
CHEBI ID93704
SCHEMBL ID1230083
MeSH IDM0541915

Synonyms (65)

Synonym
HMS1579M04
phenylethynesulfonamide
EN300-27810
HMS3269J15
BRD-K96799727-001-01-7
nsc-303580
nsc303580
64984-31-2
pifithrin-mu, >=97% (hplc), solid
OPREA1_468179
OPREA1_544600
pifithrin-mu
NCGC00162358-01
NCGC00162358-02
NCGC00162358-03
2-phenylethynesulfonamide
AKOS001417066
HMS3263J21
CHEMBL1241268
2-phenylacetylenesulfonamide
CCG-2233
BRD-K96799727-001-03-3
FT-0673769
LP01170
S2930
NCGC00261855-01
tox21_501170
SCHEMBL1230083
cambridge id 5147472
pifithrin-micro
nsc 303580
pifithrin-.mu.
ZZUZYEMRHCMVTB-UHFFFAOYSA-N
HB3025
P2048
mfcd00181531
EX-A1232
DTXSID40316450
2-phenylethyne-1-sulfonamide
CHEBI:93704
HMS3651B14
pft|i
pifithrin-|i
AS-60233
CS-0002901
HY-10940
Z56915355
pifithrin-u
SW148473-2
pifithrin-_
nsc 303580;pft|i
BCP06510
Q27165400
pifithrin-mu - cas 64984-31-2
A867775
phenylethynsulfonic acid amide
HMS3677N19
HMS3413N19
SDCCGSBI-0633799.P001
NCGC00162358-13
pftmu;2-phenylethynesulfonamide
pifithrin->m
pifithrin- mu
pft;2-phenylethynesulfonamide
AC-36838
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency7.87140.100020.879379.4328AID488773; AID588453; AID588456
ATAD5 protein, partialHomo sapiens (human)Potency27.49980.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency32.58100.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
ParkinHomo sapiens (human)Potency29.09290.819914.830644.6684AID720573
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency20.74910.016525.307841.3999AID602332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency73.07800.01262.451825.0177AID485313
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency21.33130.134610.395030.1313AID1347049
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.48160.00669.809418.4927AID1347050
ras-related protein Rab-9AHomo sapiens (human)Potency58.04790.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency22.01500.00378.618923.2809AID2660; AID2668
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency20.55240.00798.23321,122.0200AID2546; AID2551
Ataxin-2Homo sapiens (human)Potency39.81070.011912.222168.7989AID588378
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (128)

Assay IDTitleYearJournalArticle
AID513212Inhibition of p53-mediated transactivation of p21 in gamma-stimulated human SK-MEL-29 cells at 10 uM after 6 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513228Induction of Noxa gene expression in UV-induced human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513229Induction of Noxa gene expression in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889140Induction of autophagy in human DOHH-2 cells assessed as reduction in p62 expression at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889128Induction of apoptosis in human DOHH-2 cells assessed as increase in cleaved caspase-3 expression at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513185Antiapoptotic activity against TNF-alpha induced apoptosis in mouse fibroblast assessed as cell survival at 0.1 uM to 10 uM by methylene blue assay in presence of 0.5 ug/ml cycloheximidine after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513224Inhibition of p53 in human ConA cells assessed as effect on cell cycle distribution at 10 uM after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513243Binding affinity to human recombinant caspase 2 at 10 uM by cell-free system2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889118Binding affinity to ADP-bound full-length human HSP70 assessed as Cys603 adduct formation by size exclusion chromatography2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513250Binding affinity to p53 transfected in human Saos-2 cells harboring pLV-53 assessed as cytosolic p53 concentration at 10 uM after 48 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513226Induction of Puma gene expression in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889121Cytotoxicity against HEK293T cells up to 20 uM measured after 24 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889126Cytotoxicity against human MDA-MB-453 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513236Induction of Bax gene expression in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889158Up regulation of HSP90alpha expression in human DOHH-2 cells at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513238Induction of Puma gene expression in mouse thymocytes2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513183Antiapoptotic activity against TNF-alpha induced apoptosis in human WI38 cells assessed as cell survival at 0.1 uM to 10 uM after 24 hrs by methylene blue assay in presence of 0.5 ug/ml cycloheximidine2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513186Antiapoptotic activity against fas-induced apoptosis in mouse fibroblast assessed as cell survival at 0.1 uM to 10 uM by methylene blue assay in presence of 1 ug/ml cycloheximidine after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889123Cytotoxicity against human DOHH-2 cells up to 20 uM measured after 24 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513241Antiapoptotic activity against Bax gene-induced apoptosis in human 293T cells transfected with pTZV3-CMV-Bax at 10 uM after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889134Induction of apoptosis in human DOHH-2 cells assessed as increase in cleaved caspase-3 expression at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513187Inhibition of p53-mediated apoptosis in human WI38 cells assessed as cell survival at 10 uM after 24 hrs by methylene blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513227Induction of Puma gene expression in UV-induced human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513206Inhibition of p53-dependent transcription of puma in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513189Inhibition of p53-mediated apoptosis in human Saos-2 cells harboring p53 expressing lentiviral vector assessed as cell survival at 10 uM after 48 hrs by methylene blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513201Inhibition of p53-dependent transcription of puma in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889122Cytotoxicity against human Jurkat T cells up to 20 uM measured after 24 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513215Inhibition of TNFalpha induced NF-kappaB activation in human H1299 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512984Antiapoptotic activity against gamma irradiation-induced apoptosis in mouse thymocyte at 10 uM after 24 hrs by trypan blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513245Binding affinity to human recombinant caspase 9 at 10 uM by cell-free system2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513237Induction of Bax gene expression in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513219Induction of p21 mRNA expression in gamma-stimulated human SK-MEL-29 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513239Induction of Puma gene expression in gamma-induced mouse thymocytes2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513207Inhibition of p53-dependent transcription of puma in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889112GSH reactivity in pH 7.4 buffer assessed as GSH adduct formation by measuring molecular weight at 1 mM by Q-TOF LC/MS analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889161Up regulation of HSP90alpha expression in human DOHH-2 cells at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513194Inhibition of p53-mediated transactivation of promoter cyclin G in human H1299 cells at 10 uM after 48 hrs by luciferase reporter assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513210Inhibition of p53-dependent transcription of noxa in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513234Induction of Noxa gene expression in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513230Induction of Bax gene expression in UV-induced human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513213Inhibition of p53-mediated transactivation of p21 in gamma-stimulated human BJ cells at 10 uM after 6 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513253Binding affinity to p53 in gamma irradiated mouse thymocyte assessed as cytosolic Bcl-2 concentration at 10 uM after 2 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513255Binding affinity to p53 in gamma irradiated mouse thymocyte assessed as cytosolic caspase 8 concentration at 10 uM after 2 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513251Binding affinity to p53 in gamma irradiated mouse thymocyte assessed as cytosolic p53 concentration at 10 uM after 2 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513195Inhibition of p53-mediated transactivation of promoter hDM2 in human H1299 cells at 10 uM after 48 hrs by lacZ reporter assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513208Inhibition of p53-dependent transcription of bax in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513184Antiapoptotic activity against Fas-induced apoptosis in human WI38 cells assessed as cell survival at 0.1 uM to 10 uM after 24 hrs by methylene blue assay in presence of 1 ug/ml cycloheximidine2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889124Cytotoxicity against human Jurkat T cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513205Inhibition of p53-dependent transcription of noxa in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512980Binding affinity to p53 transfected in human T293 cells assessed as reduction in p53 bound-Bcl-2 at 15 uM after 48 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513200Inhibition of p53-dependent transcription of puma in UV-induced human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512979Binding affinity to p53 transfected in human T293 cells assessed as reduction in p53 bound-Bcl-xL at 15 uM after 48 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513218Induction of p21 mRNA expression in human SK-MEL-29 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513199Effect on UV-induced activation of p53 in human ConA cells assessed as beta-galactosidase activity by X-gal staining2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889116Binding affinity to ADP-bound full-length human HSP70 assessed as cysteine adduct formation at SBDalpha domain by measuring half life at 1 mM by fluorescence spectra analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID512977Binding affinity to p53 assessed as reduction in mitochondrial-bound p53 level at 25 uM2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512981Inhibition of p53-induced apoptosis in gamma irradiated mouse thymocytes at 10 uM after 24 hrs by trypan blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512982Antiapoptotic activity against dexamethasone-induced apoptosis in mouse thymocyte at 10 uM2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889113GSH reactivity in pH 7.4 buffer assessed as GSH adduct formation by measuring half life at 50 uM by near-UV absorbance spectra analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID512983Antiapoptotic activity against gamma irradiation-induced apoptosis in mouse thymocyte assessed as cytosolic Cyt c concentration at 20 uM2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513235Induction of Noxa gene expression in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889146Induction of autophagy in human DOHH-2 cells assessed as change in transformation of LC3B1 to LC3B2 expression at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889135Induction of apoptosis in human DOHH-2 cells assessed as increase in cleaved PARP expression at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889125Cytotoxicity against human DOHH-2 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889111GSH reactivity in pH 7.4 buffer assessed as GSH adduct formation at 1 mM by HPLC analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513203Inhibition of p53-dependent transcription of bax in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513202Inhibition of p53-dependent transcription of bax in UV-stimulated human MGF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513214Inhibition of p53-mediated transactivation of p21 in gamma-stimulated human thymocytes at 10 uM after 6 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513249Binding affinity to p53 transfected in human Saos-2 cells harboring pLV-53 assessed as reduction of p53 protein in mitochondria at 10 uM after 48 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512978Binding affinity to p53 assessed as reduction in mitochondrial-bound p53 level at 50 uM2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513182Antiapoptotic activity against staurosporine-induced cell death in human H1299 cells assessed as cell survival at 10 uM after 24 hrs by methylene blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889152Up regulation of HSP70 expression in human DOHH-2 cells at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513211Inhibition of p53-dependent transcription of noxa in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513188Inhibition of p53-mediated apoptosis in mouse fibroblast assessed as cell survival at 10 uM after 24 hrs by methylene blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513193Inhibition of p53-mediated transactivation of promoter bax in human H1299 cells at 10 uM after 48 hrs by luciferase reporter assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513240Protection against 8 Gy gamma radiation-induced death in mouse assessed as increase in survival at 40 mg/kg, ip2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889129Induction of apoptosis in human DOHH-2 cells assessed as increase in cleaved PARP expression at 12 uM measured after 4 to 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513231Induction of Bax gene expression in human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513209Inhibition of p53-dependent transcription of bax in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889143Induction of autophagy in human DOHH-2 cells assessed as reduction in p62 expression at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513180Inhibition of p53-dependent transactivation of p21 in gamma-stimulated human ConA cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513225Inhibition of p53 in gamma-stimulated human ConA cells assessed as effect on cell cycle distribution at 10 uM after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513181Antiapoptotic activity against staurosporine-induced cell death in human HeLa cells assessed as cell survival at 10 uM after 24 hrs by methylene blue assay2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513252Binding affinity to p53 in gamma irradiated mouse thymocyte assessed as mitochondrial p53 concentration at 10 uM after 2 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889127Cytotoxicity against human HepG2 cells measured after 72 hrs2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513233Induction of Puma gene expression in doxorubicin-induced human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513242Antiapoptotic activity against Bax gene-induced apoptosis in human HT1080 cells transfected with pTZV3-CMV-Bax at 10 uM after 24 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513244Binding affinity to human recombinant caspase 8 at 10 uM by cell-free system2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513204Inhibition of p53-dependent transcription of noxa in UV-induced human MCF7 cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889117Binding affinity to human HSP70 SBDalpha domain (537 to 610 residues) C574S mutant assessed as Cys603 adduct formation by size exclusion chromatography2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513254Binding affinity to p53 in gamma irradiated mouse thymocyte assessed as cytosolic p21 concentration at 10 uM after 2 hrs2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513223Induction of p21 mRNA expression in gamma-stimulated human thymocytes2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID512976Binding affinity to p53 assessed as reduction in mitochondrial-bound p53 level at 10 uM2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889155Up regulation of HSP70 expression in human DOHH-2 cells at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID1889103Effect on global protein ubiquitination in human DOHH-2 cells at 10 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513217Inhibition of p53-dependent transcription of puma in gamma-stimulated mouse thymocyte2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1889149Induction of autophagy in human DOHH-2 cells assessed as change in transformation of LC3B1 to LC3B2 expression at 0.5 to 12 uM measured after 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60PES derivative PESA is a potent tool to globally profile cellular targets of PES.
AID513232Induction of Puma gene expression in human U2OS cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513190Protection against 9 Gy gamma radiation-induced death in mouse assessed as increase in survival at 40 mg/kg, ip2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513221Induction of p21 mRNA expression in human BJ cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513222Induction of p21 mRNA expression in human thymocytes2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513220Induction of p21 mRNA expression in 5-fluorouracil-stimulated human BJ cells2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513216Inhibition of p53-dependent transcription of puma in mouse thymocyte2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID513246Binding affinity to human recombinant caspase 10 at 10 uM by cell-free system2006Nature chemical biology, Sep, Volume: 2, Issue:9
Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC 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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
AID1347154Primary screen GU AMC 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.
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (65)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (3.08)29.6817
2010's48 (73.85)24.3611
2020's15 (23.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.89

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.89 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index5.46 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other66 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]