(R)-Roscovitine, Calbiochem®
Supplier: MilliporeSigma
Synonyms:
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Roscovitine, (R)-2-((6-(Benzylamino)-9-isopropyl-9H-purin-2-yl)amino)butan-1-ol
A potent and selective inhibitor of cyclin-dependent kinases (cdks) that exhibits about ten-fold greater efficacy towards p34cdc2 and p33cdk2, and twenty-fold greater efficacy towards p33cdk5 relative to olomoucine (80053-494, -496)
Inhibits p34cdc2/cyclin B (IC50=650nM), p33cdk2/cyclin A (IC50=700nM), p33cdk2/cyclin E (IC50=200nM), and p33cdk5/p35 (IC50=200nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases, including ERK1 and ERK2 (IC50=34µM and 14µM respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100µM, 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.
Formula:
C₁₉H₂₆N₆O MW: 354.45 g/mol |
MDL Number:
MFCD02266401 CAS Number: 186692-46-6 |
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