Roscovitine - CAS 186692-46-6 - Calbiochem (C15-1220-898)

General description

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.

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 ^cdc2/cyclin B (IC₅₀ = 0.65 µM), p33 ^cdk2/cyclin A (IC₅₀ = 0.70 µM), p33 ^cdk2/cyclin E (IC₅₀ = 0.70 µM), and p33 ^cdk5/p35 (IC₅₀ = 0.20 µM) 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.

Biochem/physiol Actions

Cell permeable: no

Primary Target
p34^cdk1/cyclin B

Product does not compete with ATP.

Reversible: yes

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for at least 6 months at -20°C.

Other Notes

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.

Legal Information

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

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