2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine White solid. A potent 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 µM and 14 µM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µM, 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. Purity: ≥95% by HPLC. CAS 186692-46-6. Ref.: De Azevedo, W.F., et al. 1997. Eur. J. Biochem. 243, 518. Meijer, L., et al. 1997. Eur. J. Biochem. 243, 527. Meijer, L., et al. 1996. Trends Cell Biol. 6, 393. Rudolph, B., et al. 1996. EMBO J. 15, 3053.
Sold under license of U.S. Patent 6,316,456 |
