How does roscovitine work?

Roscovitine [CY-202, (R)-Roscovitine, Seliciclib] is a small molecule that inhibits cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a broad-range purine inhibitor, which inhibits CDK1, CDK2, CDK5 and CDK7, but is a poor inhibitor for CDK4 and CDK6.

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Is CDK5 inhibitor available?

The function of CDK5 in cancer cells remains unclear. Since no CDK5-specific inhibitors are available, most studies employed pan-CDK inhibitors, or dominant-negative CDK5 constructs, or anti-CDK5 shRNAs.

What is a Cdk5 inhibitor?

Cdk5 has been postulated to be a neurofilament or tau protein kinase, based on its ability to phosphorylate these proteins in vitro. Cdk5 Inhibitors offered by Santa Cruz inhibit Cdk5 and, in some cases, other cell cycle and phosphorylation related proteins.

What is the mechanism of action of roscovitine?

Roscovitine is a cell permeable reversible selective inhibitor of cyclin-dependent kinases CDK1 (cdc2), CDK2 and CDK5 (1). A purine analog, this drug competes for the binding site of ATP in the catalytic cleft. Treatment of cultured cells with roscovitine can cause cell cycle arrest or apoptosis (1-4).

Is roscovitine a CDK inhibitor?

Catalog No.S1153. Molecular Weight(MW): 354.45. Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6.

Does R-roscovitine (CYC202) affect CDK?

Roscovitine (CYC202, Seliciclib, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6.

Does roscovitine affect CDK2 activity in mesangial cells?

In mesangial cells, Roscovitine results in a dose-dependent reduction of CDK2 activity that at concentrations of 7.5, 12.5 and 25 mM, Roscovitine causes a 25, 50% and 100% decrease in CDK2 activity, respectively. [2]