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Description

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34cdk1 and p33cdk2 and twenty-fold greater efficacy towards p33cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34cdk1/cyclin B (IC50 = 650 nM), p33cdk2/cyclin A (IC50 = 700 nM), p33cdk2/cyclin E (IC50 = 700 nM), and p33cdk5/p35 (IC50 = 200 nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases including ERK1 and ERK2 (IC50 = 34 µ,M and 14 µ,M, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µ,M, including p34cdk4/cyclin D1 and p40cdk6/cyclin D2. Compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle. A 50 mM (5 mg/282 µ,l) solution of Roscovitine (Cat. No. 557364) in DMSO is also available., A potent, reversible, and selective inhibitor of cyclin-dependent kinases (cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 cdc2/cyclin B (IC50 = 0.65 µ,M), p33 cdk2/cyclin A (IC50 = 0.70 µ,M), p33 cdk2/cyclin E (IC50 = 0.70 µ,M), and p33 cdk5/p35 (IC50 = 0.20 µ,M) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as erk1 and erk2 (IC50 = 34 µ,M and 14 µ,M, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µ,M and compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.