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Biological Activity:
Roscovitine is a cell permeable reversible selective inhibitor of cyclin-dependent kinases CDK1 (cdc2), CDK2 and CDK5. 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. The IC50 for cdc2 activity is 0.65 µM in vitro.
References:
Duffin, Rodger; Leitch, Andrew E.; Sheldrake, The CDK inhibitor, R-roscovitine, promotes eosinophil apoptosis by down-regulation of Mcl-1. FEBS Letters (2009), 583(15), 2540-2546.