InSolution Roscovitine-Calbiochem

C₁₉H₂₆N₆O

354.45

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.

Reversible: yes
Primary Target
p34^cdk1/cyclin B
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
Cell permeable: no

Toxicity: Irritant (B)

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

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

Meijer, L. 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.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

liquid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

wet ice

2-8℃

5 mg in Plastic ampoule
Packaged under inert gas

10 - Combustible liquids

WGK 2

188.6 °F - (Dimethylsulfoxide)

87 ℃ - (Dimethylsulfoxide)