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Overview
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Background
Roscovitine, also known as seliciclib or CYC202, is a selective cyclin-dependent kinases (cdk), which are essential cell cycle regulators frequently involved in the deregulation of human tumors, inhibitor that potently inhibits cdc2 (cdc2/cyclin B), cdk2 (cdk2/cyclin A and cdk2/cyclin E) and cdk5 (cdk5/p35) with half maximal inhibition concentration IC50 of 0.65 μM, 0.7 μM, 0.7 μM and 0.16 μM respectively [1].
Roscovitine has been found to inhibit cellular prophase/metaphase transition at micromolar concentrations, where it inhibits progesterone-induced oocyte maturation of Xenopus oocytes and arrests starfish oocytes and sea urchin embryos in late prophase [1].
Additionally, roscovitine is capable of inhibiting extracelluar regulated kinases, erk1 and erk2, with IC50 of 34 μM and 14 μM respectively [1].[1] Meijer L, Borgne A, Mulner O, Chong JP, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36.
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