Use | Roscovitine (Seliciclib,CYC202) is an effective and selective CDK inhibitor. When acting on Cdc2, CDK2 and CDK5, the IC50 is 0.65 μM, 0.7 μM and 0.16 μM, respectively, with little inhibitory effect on CDK4/6. Phase 2. |
In vitro study | Roscovitine acts on cyclin-dependent kinases with high efficiency and high selectivity, with IC50 of 0.65 and 0.7 when acting on cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p53, respectively, 0.7 and 0.16 μm. Nanomolar Roscovitine acts on starfish oocytes and sea urchin embryos, reversibly inhibits the transformation during the anterior middle period, and acts on the Xenopus laevis egg extract in vitro, inhibiting the activity of M-phase promoting factor and in vitro DNA synthesis, and inhibit the proliferation of mammalian cell lines, IC50 is 16 M. Roscovitine at concentrations of 7.5, 12.5, and 25 mM acted on mesangial cells resulting in a 25,50, and 100% decrease in CDK2 activity, respectively, in a dose-dependent manner. Recent studies have shown that Roscovitine acts on Dicostelium discoidosa to inhibit cdk5 kinase activity, cell proliferation, multicellular development, and cdk5 nuclear transport, without affecting cdk5 protein expression. |