557364

Roscovitine

InSolution, ≥95%, inhibitor of cyclin-dependent kinases (CDKs)

• Synonym(s): InSolution Roscovitine
• Empirical Formula (Hill Notation): C₁₉H₂₆N₆O
• Molecular Weight: 354.45
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• shipped in: wet ice
• storage temp.: 2-8°C

Description

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.

Biochem/physiol Actions

Cell permeable: no

Primary Target
p34^cdk1/cyclin B

Product competes with ATP.

Reversible: yes

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

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

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.

Other Notes

Meijer, L. 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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 2
• Flash Point(F): 188.6 °F - (Dimethylsulfoxide)
• Flash Point(C): 87 °C - (Dimethylsulfoxide)