Chemical Name: (2R)-2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol
Biological ActivityRoscovitine is a cyclin-dependent kinase (cdk) inhibitor. Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). Selective for cdks over a wide range of related kinases including ERK1 and ERK2. Arrests L1210 cells in G1 phase. Inhibits phosphorylation of vimentin in vivo. Antimitotic.
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How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
Jorda et al.
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.
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