Potent, selective inhibitor of cyclin-dependent kinases (cdk). Inhibits cdc2/cyclin B (IC50
= 650 nM), cdk2/cyclin A (IC50
= 700 nM), cdk2/cyclin E (IC50
= 700 nM), cdk5 / p35 (IC50
= 160 nM) and is selective over cdk4/cyclin D1 and cdk6/cyclin D3 (IC50
> 100 μ
M). Also selective over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1
phase. Inhibits phosphorylation of vimentin in vivo
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Inhibition of cyclin-dependent kinases by purine analogues.
De Azevedo et al.
Chemical inhibitors of cyclin-dependent kinases.
Trends Cell.Biol., 1996;6:393
Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5.
Meijer et al.