Roscovitine

ChEBI: 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1 and p33^cdk2 and twenty-fold greater efficacy towards p33^cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀ = 650 nM), p33^cdk2/cyclin A (IC₅₀ = 700 nM), p33^cdk2/cyclin E (IC₅₀ = 700 nM), and p33^cdk5/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 μM and 14 μM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 μM, including p34^cdk4/cyclin D1 and p40^cdk6/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 μl) solution of Roscovitine (Cat. No. 557364) in DMSO is also available.

Roscovitine a derivative of olomoucine which is isolated from Raphanus sativus isunder clinical trials (Shoeb 2006).