|Synonyms||Flavopiridol; HMR 1275.|
|Description||Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis.|
|Current Developer||Sanofi-Aventis Inc.|
KH-CB19, a CLK1/CLK4 inhibitor, has been found to probably restrain the phosphorylation of serine- and arginine-rich (SR) proteins. IC50: 20 nM for CLK1.
Dinaciclib, also known as SCH727965, is a potent CDK inhibitor with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases ...
SU 9516 is a potent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively...
SNS-032, also known as BMS-387032, is a 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. ...
Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by p...
NG 52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p (IC50s = 7 and 2 µM, respec...
LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively. Phase 3.
RGB-286638 is a novel CDK inhibitor. It inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. It demonstrated eq...
PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. Although toxicity was acceptable at initial dos...
R547 is orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI R547 selectively binds to an...
PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication.
Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway,...
Ca2+ Channel Agonist 1
A Ca2+ Channel Agonist that selectively acting on N-type Ca2+ channel and also be found to restrain the cdk activity at some extent. IC50: 14.23 uM (EC50, Ca2+ ...
AT7519 is an ATP competitive CDK inhibitor with a Ki value of 38 nM for CDK1. AT7519 is inactive against all non-CDK kinases with the exception of GSK3β (IC50 =...
THZ1-R, with the potential to treat Triple-negative breast cancer (TNBC), it is a potent and selective CDK7 inhibitor but has instability in vivo.
Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activati...
CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a mean LD50 value of 0.08μM ± 0.10 μM following exposure to drug for 48h. In contrast, norm...
WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity. The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i...
THZ2, an analog of THZ1, with the potential to treat Triple-negative breast cancer (TNBC), it is a potent and selective CDK7 inhibitor which overcomes the insta...
ON123300, a dihydropyrido[2,3-d]pyrimidine derivative, has been found to be an effective multikinase inhibitor that could be probably used against brain tumor a...