Purvalanol A is a potent CDK inhibitor. It inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, and 75 nM, respectively. It also inhibits cdc28 (S. cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with an average GI50 of 2 μM. It is a 2.5-fold more potent inhibitor of CDK2, and potently inhibits DYRK1A and other protein kinases in the low micromolar range. It selectively inhibits the phosphorylation of cellular proteins and prevents the increases of cyclins D and E during serum-induced G1 phase progression.
- Potent CDK inhibitor
- Inhibits various cyclin-dependent kinases (CDKs)
- Exhibits cytotoxic effects on various cancer cell lines
- Selectively inhibits the phosphorylation of cellular proteins
- Prevents increases of cyclins D and E during G1 phase progression