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Sigma-Aldrich

Roscovitine

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

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Synonym(s):
InSolution Roscovitine
Empirical Formula (Hill Notation):
C19H26N6O
Molecular Weight:
354.45

Quality Level

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

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
p34cdk1/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

Storage Class

10 - Combustible liquids

wgk_germany

WGK 2

flash_point_f

188.6 °F - (Dimethylsulfoxide)

flash_point_c

87 °C - (Dimethylsulfoxide)


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