Biochem/physiol Actions

Cell permeable: no

Reversible: yes

Product competes with ATP.

Target IC₅₀: 650 nM, 700 nM, 700 nM, and 200 nM against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, and p33cdk5/p35, respectively

Primary Targetp34^cdk1/cyclin B

General description

A potent and selective inhibitor of cyclin-dependent kinases (Cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 Cdc2/cyclin B (IC₅₀ = 650 nM), p33 Cdk2/cyclin A (IC₅₀ = 700 nM), p33 Cdk2/cyclin E (IC₅₀ = 700 nM), and p33 Cdk2/p35 (IC₅₀ = 200 nM) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as 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 and compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G₁/S and G₂/M phases of the cell cycle.

Legal Information

Sold under license of U.S. Patent 6,316,456.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Meijer, L. 1996. Trends Cell Biol.6, 393.Rudolph, B., et al. 1996. EMBO J.15, 3053.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Physical form

A 50 mM (5 mg/282 µl) solution of Roscovitine (Cat. No. 557360) in DMSO.

Reconstitution

Following initial use, aliquot and freeze (-20°C). Once opened, the DMSO aliquots are stable for up to 6 months at -20°C.

Warning

Toxicity: Irritant (B)