apratoxin a profile

apratoxin A: a potent cytotoxin with a novel skeleton, has been isolated from the marine cyanobacterium Lyngbya majuscula Harvey ex Gomont; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

apratoxin A : An aprotoxin having the common aprotoxin cyclodepsipeptide skeleton where the isoleucyl residue carries an N-methyl substituent and the side-chain adjacent to the lactone is tert-butyl. [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]

ID Source	ID
PubMed CID	6326668
CHEMBL ID	501696
CHEBI ID	35212
SCHEMBL ID	63138
MeSH ID	M0408631

Synonym
apratoxin a
7'''.1,4-anhydro(n-{3-[2-(3,7-dihydroxy-5,8,8-trimethylnonan-2-yl)-4,5-dihydro-1,3-thiazol-4-yl]-2-methylpropenoyl}-o-methyl-l-tyrosyl-n-methyl-l-alanyl-n-methyl-l-isoleucyl-l-proline)
n-((2e)-3-((4s)-4,5-dihydro-2-((1s,2s,4s,6s)-2,6-dihydroxy-1,4,7,7-tetramethyloctyl)-4-thiazolyl)-2-methyl-1-oxo-2-propenyl)-o-methyl-l-tyrosyl-n-methyl-l-alanyl-n-methyl-l-isoleucyl-l-proline-(4-1(6))-lactone
(2s,3s,5s,7s,10s,16s,19s,22s,25e,27s)-16-[(2s)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-(4-methoxybenzyl)-2,5,17,19,20,25-hexamethyl-8-oxa-29-thia-14,17,20,23,30-pentaazatricyclo[25.2.1.0(10,14)]triaconta-1(30),25-diene-9,15,18,21,24-pentone
350791-64-9
CHEBI:35212 ,
CHEMBL501696
SCHEMBL63138
DTXSID5040419
Q4781819
EX-A7019
(2s,3s,5s,7s,10s,16s,19s,22s,25e,27s)-16-[(2s)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-[(4-methoxyphenyl)methyl]-2,5,17,19,20,25-hexamethyl-8-oxa-29-thia-14,17,20,23,30-pentazatricyclo[25.2.1.010,14]triaconta-1(30),25-diene-9,15,18,21,24-pentone
XA177351
CS-0634873
HY-P3989
AKOS040750549

Excerpt	Reference	Relevance
"Apratoxin A is a potent anticancer natural product whose key polyketide fragment constitutes a considerable challenge for organic synthesis, with five prior syntheses requiring 12 to 20 steps for its preparation. "	( Catalysis Driven Six-Step Synthesis of Apratoxin A Key Polyketide Fragment. Quintard, A; Rodriguez, J; Shao, N, 2022)	2.43
"Apratoxin A is a natural product with potent antiproliferative activity against many human cancer cell lines. "	( Apratoxin A Shows Novel Pancreas-Targeting Activity through the Binding of Sec 61. Agoulnik, S; Akare, S; Chen, Z; Choi, HW; Condon, K; Gerwick, WH; Huang, KC; Jiang, Y; Kolber-Simonds, D; Kotake, Y; Mathieu, S; Nomoto, K; Shen, Y; Shimizu, H; Tendyke, K; Uenaka, T; Woodall-Jappe, M; Wu, KM; Zhu, X, 2016)	3.32
"Apratoxin A is a cytotoxic natural product that prevents the biogenesis of secretory and membrane proteins. "	( Apratoxin Kills Cells by Direct Blockade of the Sec61 Protein Translocation Channel. Almaliti, J; Dunyak, BM; Gerwick, WH; Gestwicki, JE; Kellosalo, J; Paatero, AO; Paavilainen, VO; Taunton, J, 2016)	1.88
"Apratoxin A is a potent cytotoxic marine natural product that rapidly inhibits signal transducer and activator of transcription (STAT) 3 phosphorylation by an undefined mechanism. "	( Apratoxin a reversibly inhibits the secretory pathway by preventing cotranslational translocation. Law, BK; Liu, Y; Luesch, H, 2009)	3.24

Role	Description
metabolite	Any intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
[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]

Class	Description
apratoxin	A class of marine cyanobacterial cyclodepsipeptides containing discrete polypeptide and polyketide domains.
1,3-thiazoles
[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]

Bioassays (229)

Assay ID	Title	Year	Journal	Article
AID512781	Cytotoxicity against human K562 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512862	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512914	Inhibition of apoptosis in human U2OS cells transfected with mouse Rela cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512843	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512815	Cytotoxicity against human IGROV1 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658129	Toxicity in human HCT116 cells xenografted nu/nu mouse assessed as mortality at > 0.375 mg/kg, ip measured post compound withdrawal	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512780	Cytotoxicity against human HL-60(TB) cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512821	Cytotoxicity against human 786-0 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512957	Inhibition of FGFR1 signaling-induced STAT3-luciferase activity in human U2OS cells transfected with FGFR1 variant 3 cDNA at 15 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512806	Cytotoxicity against human U251 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512801	Cytotoxicity against human SF268 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512805	Cytotoxicity against human SNB75 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512938	Cell cycle arrest in human U2OS cells overexpressing mouse Kras2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512684	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human HUVEC cells at 100 nM by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512823	Cytotoxicity against human Caki1 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512910	Cytotoxicity against resting human CD4+ T cell assessed as cell viability after 3 days by fluorescence detection method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512846	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512837	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512696	Inhibition of FGFR-mediated distal pectoral fin development in Zebrafish embryo at 40 uM after 72 hrs post fertilization stage by in situ hybridization method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658123	Irreversible toxicity in human HCT116 cells xenografted nu/nu mouse at > 0.375 mg/kg, ip	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512920	Inhibition of apoptosis in human U2OS cells transfected with human EBAG9 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512960	Inhibition of FGFR4 signaling-induced STAT3-luciferase activity in human U2OS cells transfected with FGFR4 variant 2 cDNA at 15 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512831	Cytotoxicity against human NCI/ADR-RES cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512907	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 50 nM by FACS analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658110	Inhibition of VEGF-A secretion in human HCT116 cells after 12 hrs	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512697	Inhibition of FGFR-mediated posterior mesoderm development in Zebrafish embryo at 700 nM after 72 hrs post fertilization stage by in situ hybridization method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512868	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446339	Growth inhibition of human U87MG cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512828	Cytotoxicity against human PC3 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512685	Inhibition of FGFR signaling-induced STAT3 ser727 phosphorylation in human HUVEC cells at 10 nM after 1 -4 hrs by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512928	Cell cycle arrest in human U2OS cells overexpressing mouse Fgfr1 assessed as accumulation at S phase at 15 nM after 48 hrs by CMV-GFP reporter assay method (Rvb = 33%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID405550	Antiproliferative activity against human HT29 cells after 48 hrs by MTT assay	2008	Journal of natural products, Jun, Volume: 71, Issue:6	Apratoxin E, a cytotoxic peptolide from a guamanian collection of the marine cyanobacterium Lyngbya bouillonii.
AID512850	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512844	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512836	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512854	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658125	Toxicity in human HCT116 cells xenografted nu/nu mouse assessed as mortality at > 0.375 mg/kg, ip	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512816	Cytotoxicity against human OVCAR-3 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512878	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512787	Cytotoxicity against human HOP62 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512913	Cytotoxicity against human U2OS cells assessed as cell viability by MTT assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512883	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512818	Cytotoxicity against human OVCAR5 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512792	Cytotoxicity against human NCI-H460 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512904	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase after 24 hrs by FACS analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512908	Induction of apoptosis in human U2OS cells assessed as caspase3 dependent cleavage of Ac-DEVD-pNA at 50 nM after 6-48 hrs by calorimetry relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512871	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512943	Cell cycle arrest in human U2OS cells overexpressing mouse Ppp1cc assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512882	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512789	Cytotoxicity against human NCI-H226 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512807	Cytotoxicity against human LOXIMVI cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446335	Growth inhibition of human BxPC3 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID1446336	Growth inhibition of human A549 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512893	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512827	Cytotoxicity against human UO31 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512784	Cytotoxicity against human SR cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512964	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512948	Cell cycle arrest in human U2OS cells overexpressing human AIP assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658128	Toxicity in human HCT116 cells xenografted nu/nu mouse assessed as body weight loss at > 0.375 mg/kg, ip measured post compound withdrawal	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512886	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512959	Inhibition of FGFR2 signaling-induced STAT3-luciferase activity in human U2OS cells transfected with FGFR2 variant 2 cDNA at 15 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512840	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512783	Cytotoxicity against human RPMI8266 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512855	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512925	Inhibition of apoptosis in human U2OS cells transfected with human GDAP1L1 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446342	Growth inhibition of human 786-O cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512894	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512802	Cytotoxicity against human SF295 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512934	Cell cycle arrest in human U2OS cells overexpressing mouse Ets1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512689	Inhibition of FGFR-mediated mkp3 mRNA expression in Zebrafish embryo mid-hind brain boundary at 700 nM by in situ hybridization analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512879	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512902	Cell cycle arrest in human U2OS cells assessed as accumulation at at S phase at 50 nM after 48 hrs by FACS analysis (Rvb = 37.3%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512906	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 5 nM by FACS analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512970	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 0.32 to 1000 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512813	Cytotoxicity against human UACC257 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446344	Drug metabolism in mouse liver microsomes after 35 mins in presence of NADPH by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512814	Cytotoxicity against human UACC62 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512809	Cytotoxicity against human M14 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512793	Cytotoxicity against human NCI-H522 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512942	Cell cycle arrest in human U2OS cells overexpressing mouse Map2k2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512804	Cytotoxicity against human SNB19 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512822	Cytotoxicity against human ACHN cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658127	Irreversible toxicity in human HCT116 cells xenografted nu/nu mouse at > 0.375 mg/kg, ip measured post compound withdrawal	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512889	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512824	Cytotoxicity against human RXF393 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446340	Growth inhibition of human SKOV3 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512874	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512803	Cytotoxicity against human SF539 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512847	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512952	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human U2OS cells overexpressing FGFR1 at 50 nM after 1 hr by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512782	Cytotoxicity against human MOLT4 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658109	Cytotoxicity against human HCT116 cells after 48 hrs	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512841	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512876	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID405551	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	2008	Journal of natural products, Jun, Volume: 71, Issue:6	Apratoxin E, a cytotoxic peptolide from a guamanian collection of the marine cyanobacterium Lyngbya bouillonii.
AID512795	Cytotoxicity against human HCC2998 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512826	Cytotoxicity against human TK10 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512839	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512901	Cell cycle arrest in human U2OS cells assessed as accumulation at S phase at 5 nM after 48 hrs by FACS analysis (Rvb = 37.3%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512812	Cytotoxicity against human SK-MEL-5 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512927	Cell cycle arrest in human U2OS cells overexpressing mouse Fgfr1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method (Rvb = 58%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446333	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by WST8 assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512962	Cytotoxicity against human HUVEC cells at 10 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512885	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512866	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512852	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512897	Cell cycle arrest in human U2OS cells assessed as accumulation at S phase at 5 nM after 24 hrs by FACS analysis (Rvb = 37.3%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512909	Cytotoxicity against activated human CD4+ T cells assessed as cell viability after 5 days by fluorescence detection method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512686	Inhibition of FGFR signaling-induced STAT3 ser727 phosphorylation in human HUVEC cells at 100 nM after 1 -4 hrs by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512810	Cytotoxicity against human SK-MEL-2 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512872	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512877	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512945	Cell cycle arrest in human U2OS cells overexpressing mouse Pbxip1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512832	Cytotoxicity against human MDA-MB-231 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512884	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512955	Inhibition of FGFR signaling-induced STAT3 transcriptional activity in human U2OS cells at 0.1 to 1000 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1651710	Inhibition of protein biogenesis in human HCT116 cells assessed as reduction in total protein level preincubated for 30 mins followed by addition of 35S-labeled methionine/cysteine and measured after 90 mins by autoradiography	2020	Journal of natural products, 04-24, Volume: 83, Issue:4	Kendomycin Cytotoxicity against Bacterial, Fungal, and Mammalian Cells Is Due to Cation Chelation.
AID512833	Cytotoxicity against human MDA-MB-435 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512880	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512688	Inhibition of FGFR-mediated mkp3 mRNA expression in Zebrafish embryo tailbud region at 700 nM by in situ hybridization analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512859	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512881	Antitumor activity against human HT-29 cells assessed as down-regulation of GTSE1 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512903	Cell cycle arrest in human U2OS cells assessed as accumulation at sub-G1 phase at 50 nM after 48 hrs by FACS analysis relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512946	Cell cycle arrest in human U2OS cells overexpressing human RNPC2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512887	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512698	Inhibition of FGFR-mediated posterior mesoderm development in Zebrafish embryo at 40 uM after 72 hrs post fertilization stage by in situ hybridization method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512891	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512870	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446341	Growth inhibition of human HEC6 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512917	Inhibition of apoptosis in human U2OS cells transfected with human BCL2 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512811	Cytotoxicity against human SK-MEL-28 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512851	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512867	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446345	Drug metabolism in human liver microsomes after 35 mins in presence of NADPH by LC-MS/MS analysis	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512905	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase after 48 hrs by FACS analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512861	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446343	Growth inhibition of human MCF7 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID1651711	Inhibition of protein biogenesis in human HCT116 cells assessed as reduction in secreted protein level preincubated for 30 mins followed by addition of 35S-labeled methionine/cysteine and measured after 90 mins by autoradiography	2020	Journal of natural products, 04-24, Volume: 83, Issue:4	Kendomycin Cytotoxicity against Bacterial, Fungal, and Mammalian Cells Is Due to Cation Chelation.
AID512860	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512937	Cell cycle arrest in human U2OS cells overexpressing human KRAS2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512898	Cell cycle arrest in human U2OS cells assessed as accumulation at S phase at 50 nM after 24 hrs by FACS analysis (Rvb = 37.3%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512838	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID767882	Cytotoxicity against human NCI-H460 cells after 48 hrs by MTT assay	2013	Journal of natural products, Sep-27, Volume: 76, Issue:9	Apratoxin H and apratoxin A sulfoxide from the Red Sea cyanobacterium Moorea producens.
AID512857	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512790	Cytotoxicity against human NCI-H23 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512798	Cytotoxicity against human HT-29 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512922	Inhibition of apoptosis in human U2OS cells transfected with human MGC2714 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512932	Cell cycle arrest in human U2OS cells overexpressing human FGFR2 transcript variant 2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512935	Cell cycle arrest in human U2OS cells overexpressing mouse Etv4 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID405552	Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay	2008	Journal of natural products, Jun, Volume: 71, Issue:6	Apratoxin E, a cytotoxic peptolide from a guamanian collection of the marine cyanobacterium Lyngbya bouillonii.
AID512972	Inhibition of FGFR signaling-induced ngiogenesis in human HUVEC cells assessed as decrease in mesh-like structure formation at 0.32 to 1000 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512939	Cell cycle arrest in human U2OS cells overexpressing mouse Rras2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512683	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human HUVEC cells at 10 nM by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512954	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human U2OS cells overexpressing FGFR1 at 1-50 nM by Western blot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512785	Cytotoxicity against human A549 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512849	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512915	Inhibition of apoptosis in human U2OS cells transfected with human RELA cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512830	Cytotoxicity against human MCF7 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512786	Cytotoxicity against human EKVX cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512936	Cell cycle arrest in human U2OS cells overexpressing human ELF5 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512796	Cytotoxicity against human HCT116 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446338	Growth inhibition of human MKN74 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512950	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human U2OS cells at 50 nM by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512875	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512918	Inhibition of apoptosis in human U2OS cells transfected with human REL cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512930	Cell cycle arrest in human U2OS cells overexpressing human FGFR1 transcript variant 3 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512961	Antiproliferative activity against human U2OS cells expressing constitutively active Stat3 mutant after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512911	Cytotoxicity against activated human CD4+ T cell assessed as cell viability after 5 days by fluorescence detection method relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512941	Cell cycle arrest in human U2OS cells overexpressing mouse Mcl1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512791	Cytotoxicity against human NCI-H322M cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512845	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512864	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512794	Cytotoxicity against human COLO205 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512797	Cytotoxicity against human HCT15 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512842	Antitumor activity against human HT-29 cells assessed as upregulation of DDIT4 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512900	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 50 nM after 48 hrs by FACS analysis (Rvb = 49.8%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512933	Cell cycle arrest in human U2OS cells overexpressing human FGFR4 transcript variant 2 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512926	Inhibition of apoptosis in human U2OS cells transfected with mouse Rbmx cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512956	Inhibition of FGFR1 signaling-induced STAT3-luciferase activity in human U2OS cells transfected with Fgfr1 cDNA at 15 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512808	Cytotoxicity against human MALME-3M cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512896	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 50 nM after 24 hrs by FACS analysis (Rvb = 49.8%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512949	Cell cycle arrest in human U2OS cells overexpressing human TKTL1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512931	Cell cycle arrest in human U2OS cells overexpressing human FGFR1 transcript variant 8 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512958	Inhibition of FGFR1 signaling-induced STAT3-luciferase activity in human U2OS cells transfected with FGFR1 variant 8 cDNA at 15 nM after 24 hrs by luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512940	Cell cycle arrest in human U2OS cells overexpressing human BCL2A1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446337	Growth inhibition of human HuH7 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512923	Inhibition of apoptosis in human U2OS cells transfected with human MAFB cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512895	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 5 nM after 24 hrs by FACS analysis (Rvb = 49.8%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512817	Cytotoxicity against human OVCAR4 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512892	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512825	Cytotoxicity against human SN12C cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512924	Inhibition of apoptosis in human U2OS cells transfected with human RIOK2 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512853	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512834	Cytotoxicity against human T47D cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512953	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human U2OS cells overexpressing FGFR1 after 4 hrs by Western blot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512929	Cell cycle arrest in human U2OS cells overexpressing mouse Fgfr1 assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512899	Cell cycle arrest in human U2OS cells assessed as accumulation at G1 phase at 5 nM after 48 hrs by FACS analysis (Rvb = 49.8%)	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512947	Cell cycle arrest in human U2OS cells overexpressing human RIT assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID1446334	Growth inhibition of human HCT116 cells after 72 hrs by Cell-Titer Glo assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Conformation-Based Design and Synthesis of Apratoxin A Mimetics Modified at the α,β-Unsaturated Thiazoline Moiety.
AID512848	Antitumor activity against human HT-29 cells assessed as upregulation of HSPA1A mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512687	Inhibition of FGFR-mediated mkp3 mRNA expression in Zebrafish embryo dorsal forebrain at 700 nM by in situ hybridization analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512873	Antitumor activity against human HT-29 cells assessed as down-regulation of CCNE2 mRNA expression at 2 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512963	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512820	Cytotoxicity against human SKOV3 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512856	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 10 nM after 6 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512944	Cell cycle arrest in human U2OS cells overexpressing mouse Cherp assessed as accumulation at G1 phase at 15 nM after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512951	Inhibition of FGFR signaling-induced STAT3 ser727 phosphorylation in human U2OS cells at 50 nM after 1 to 24 hrs by immunoblot analysis	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512919	Inhibition of apoptosis in human U2OS cells transfected with human BIRC4 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512819	Cytotoxicity against human OVCAR8 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512829	Cytotoxicity against human DU145 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512865	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512800	Cytotoxicity against human SW620 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512869	Antitumor activity against human HT-29 cells assessed as down-regulation of CDC25A mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512788	Cytotoxicity against human HOP92 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512968	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in cell migration at 0.32 to 1000 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512969	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in capillary tube visibility at 0.32 to 1000 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID658124	Toxicity in human HCT116 cells xenografted nu/nu mouse assessed as body weight loss at > 0.375 mg/kg, ip	2011	ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11	Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
AID512835	Antitumor activity against human HT-29 cells assessed as upregulation of RASSF4 mRNA expression at 2 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512888	Antitumor activity against human HT-29 cells assessed as upregulation of KCNK10 mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512916	Inhibition of apoptosis in human U2OS cells transfected with mouse Prkaca cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512695	Inhibition of FGFR-mediated distal pectoral fin development in Zebrafish embryo at 700 nM after 72 hrs post fertilization stage by in situ hybridization method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512863	Antitumor activity against human HT-29 cells assessed as down-regulation of TAL1 mRNA expression at 2 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512921	Inhibition of apoptosis in human U2OS cells transfected with mouse Egr2 cDNA assessed as cell viability after 48 hrs by CMV-GFP reporter assay method	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512799	Cytotoxicity against human KM12 cells by sulforhodamine B assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512912	Cytotoxicity against human U2OS cells assessed as cell viability by CMV-luciferase reporter assay	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512890	Antitumor activity against human HT-29 cells assessed as upregulation of MGC4504 mRNA expression at 10 nM after 3 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512858	Antitumor activity against human HT-29 cells assessed as down-regulation of RAB11B mRNA expression at 10 nM after 12 hrs relative to control	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512971	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in closed polygon formation at 0.32 to 1000 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
AID512965	Inhibition of FGFR signaling-induced angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at >100 nM after 14 hrs	2006	Nature chemical biology, Mar, Volume: 2, Issue:3	A functional genomics approach to the mode of action of apratoxin A.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	14 (45.16)	29.6817
2010's	14 (45.16)	24.3611
2020's	3 (9.68)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (6.45%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	29 (93.55%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
pd 173074 [no description available]	2.03	1	aromatic amine; biaryl; dimethoxybenzene; pyridopyrimidine; tertiary amino compound; ureas	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; fibroblast growth factor receptor antagonist
safrole Safrole: A member of the BENZODIOXOLES that is a constituent of several VOLATILE OILS, notably SASSAFRAS oil. It is a precursor in the synthesis of the insecticide PIPERONYL BUTOXIDE and the drug N-methyl-3,4-methylenedioxyamphetamine (MDMA).. safrole : A member of the class of benzodioxoles that is 1,3-benzodioxole which is substituted by an allyl group at position 5. It is found in several plants, including black pepper, cinnamon and nutmeg, and is present in several essential oils, notably that of sassafras. It has insecticidal properties and has been used as a topical antiseptic. Although not thought to pose a significant carcinogenic risk to humans, findings of weak carcinogenicity in rats have resulted in the banning of its (previously widespread) use in perfumes and soaps, and as a food additive.	2.08	1	benzodioxoles	flavouring agent; insecticide; metabolite; plant metabolite
mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.	2.15	1	mitomycin	alkylating agent; antineoplastic agent
serine Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.	2.05	1	L-alpha-amino acid; proteinogenic amino acid; serine family amino acid; serine zwitterion; serine	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
adenosine monophosphate Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.	2.11	1	adenosine 5'-phosphate; purine ribonucleoside 5'-monophosphate	adenosine A1 receptor agonist; cofactor; EC 3.1.3.1 (alkaline phosphatase) inhibitor; EC 3.1.3.11 (fructose-bisphosphatase) inhibitor; fundamental metabolite; micronutrient; nutraceutical
cycloheximide Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.	2.25	1	antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol	anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor
sulfoxide sulfoxide: synergistic insecticide for use with pyrethrum, allethrin, rotenone, ryania, etc.; RN given refers to parent cpd; structure. sulfoxide : An organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H).	7.08	1	benzodioxoles
oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.	4.41	6	1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
thiazoles [no description available]	4.27	5	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
rhenium Rhenium: A metal, atomic number 75, atomic weight 186.207, symbol Re.	2.05	1	manganese group element atom
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	2.04	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
reveromycin a reveromycin A: from an actinomycete strain; structure given in first source; inhibits the mitogenic activity of the epidermal growth factor	2.03	1
proline Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.	2.01	1	amino acid zwitterion; glutamine family amino acid; L-alpha-amino acid; proline; proteinogenic amino acid	algal metabolite; compatible osmolytes; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
thapsigargin Thapsigargin: A sesquiterpene lactone found in roots of THAPSIA. It inhibits SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES.. thapsigargin : An organic heterotricyclic compound that is a hexa-oxygenated 6,7-guaianolide isolated fron the roots of Thapsia garganica L., Apiaceae. A potent skin irritant, it is used in traditional medicine as a counter-irritant. Thapsigargin inhibits Ca(2+)-transporting ATPase mediated uptake of calcium ions into sarcoplasmic reticulum and is used in experimentation examining the impacts of increasing cytosolic calcium concentrations.	2.17	1	butyrate ester; organic heterotricyclic compound; sesquiterpene lactone	calcium channel blocker; EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor
dactinomycin Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)	2.04	1	actinomycin	mutagen
benzyloxycarbonylleucyl-leucyl-leucine aldehyde benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.	2.25	1	amino aldehyde; carbamate ester; tripeptide	proteasome inhibitor
hectochlorin hectochlorin: structure in first source	2.08	1
methyl-thiohydantoin-tryptophan methyl-thiohydantoin-tryptophan: structure in first source	3.13	1	organonitrogen compound; organooxygen compound
su 5402 SU 5402: structure given in first source. SU5402 : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 3-(2-carboxyethyl)-4-methyl-1H-pyrrol-2-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.	2.03	1
sanglifehrin a sanglifehrin A: binds cyclophilin A; isolated from Streptomyces; structure in first source	3.31	1
kendomycin kendomycin: structure in first source	2.25	1	benzofurans
jasplakinolide jasplakinolide: cyclodepsipeptide isolated from marine sponge Jaspis; active against Candida; RN refers to 2S-(2R,4E,6S,8R*)-isomer; structure in first source. jaspamide : A cyclodepsipeptide isolated from Jaspis splendens and has been shown to exhibit antineoplastic activity. It is an actin polymerization and stabilization inducer.	3.31	1	cyclodepsipeptide; phenols	actin polymerisation inducer; animal metabolite; antifungal agent; antineoplastic agent; apoptosis inducer; marine metabolite; neuroprotective agent
erastin erastin: an antineoplastic agent; structure in first source. erastin : A member of the class of quinazolines that is quinazolin-4(3H)-one in which the hydrogens at positions 2 and 3 are replaced by 1-{4-[(4-chlorophenoxy)acetyl]piperazin-1-yl}ethyl and 2-ethoxyphenyl groups, respectively. It is an inhibitor of voltage-dependent anion-selective channels (VDAC2 and VDAC3) and a potent ferroptosis inducer.	3.13	1	aromatic ether; diether; monochlorobenzenes; N-acylpiperazine; N-alkylpiperazine; quinazolines; tertiary carboxamide	antineoplastic agent; ferroptosis inducer; voltage-dependent anion channel inhibitor
telomestatin telomestatin: isolated from Spreptomyces anulatus; structure in first source	3.31	1
largazole largazole: an antiproliferative agent from Symploca; structure in first source	3.31	1
coibamide a coibamide A: from the Panamanian marine cyanobacterium Leptolyngbya sp.; structure in first source	2.88	3
lyngbyabellin b lyngbyabellin B: from the marine cyanobacterium Lyngbya majuscula; structure in first source	2.08	1

Condition	Relationship Strength	Studies
Benign Neoplasms [description not available]	3.9	4
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.9	4
Breast Cancer [description not available]	2.45	2
Astrocytoma, Grade IV [description not available]	2.13	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.45	2
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	2.13	1
Bone Cancer [description not available]	2.03	1
Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES.	2.03	1
Adenocarcinoma, Basal Cell [description not available]	2	1
Cancer of Colon [description not available]	2	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	2	1
Colonic Neoplasms Tumors or cancer of the COLON.	2	1

apratoxin a

Description

Cross-References

Synonyms (16)

Research Excerpts

Overview

Roles (2)

Drug Classes (2)

Bioassays (229)

Research

Studies (31)

Market Indicators

Research Demand Index: 22.75

Study Types

apratoxin a

Description

Cross-References

Synonyms (16)

Research Excerpts

Overview

Roles (2)

Drug Classes (2)

Bioassays (229)

Research

Studies (31)

Market Indicators

Research Demand Index: 22.75

Study Types

Related Drugs (27)

Related Conditions (12)