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Flavopiridol HCl
Cat No.
CEI-0294
Description
Flavopiridol (Alvocidib) can inhibit CDK1, CDK2, CDK4, CDK5, CDK6, and CDK9 with IC50 of
CAS No.
146426-40-6
Molecular Weight
401.84
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
CDK1/CDK2, CDK4/CDK5/CDK6, CDK9
Molecular Formula
C21H20ClNO5
Chemical Name
2-(2-chlorophenyl)-5,7-dihydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-one hydrochloride
Solubility
DMSO 88 mg/mL Water 37 mg/mL Ethanol
In vitro
Flavopiridol (L86-8275), which is a potent cyclin-dependent kinase (CDK) inhibitor, can inhibit cell cycle progression in either G1 or G2. In vitro, flavopiridol can inhibit CDK2 with IC50 of 300 nM. Similarly, flavopiridol inhibited CDK4-cyclin D1 in vitro. As an ATP competitive inhibitor, flavopiridol can recombinant CDK4-cyclin D1 with Ki value of 65 nM. Flavopiridol inactivated positive transcription elongation factor b (P-TEFb), a kinase that phosphorylates and activates RNA poly-merase II (RNAP II), through the inhibition of CDK7 and CDK9. This inactivation resulted in decreased phosphorylation and transcriptional activity of RNAP II. Inhibition of P-TEFb led to decreased RNAP II activity, decreased gene transcription, down-modulation of a variety of antiapoptotic proteins such as Mcl-1,and induction of apoptosis. Flavopiridol can inhibit cell proliferation of MDA-MB-468 by inducing cell cycle arrest both in G1 and G2.
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