flavopiridol

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

Flavopiridol hydrochloride (MDL 107826A) 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. This agent is also a competitive inhibitor of adenosine triphosphate activity.

CDK9/10/GSK3β-IN-1 is a kinase inhibitor (Flavopiridol analogue) that effectively inhibits HsGSK3β, HsCDK9/CyclinT, HsCDK5/p25 and HsCDK2/CyclinA with IC50 values of 59 nM, 64 nM, 1.093 μM and 1.725 μM, respectively. CDK9/10/GSK3β-IN-1 exhibited comparable or higher anti-cancer cell activity than Flavopiridol and showed high anti-proliferative activity against up to seven cancer cell lines in vitro.