(R)-Roscovitine

[6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine]

Prod. # now: BML-CC205

Potent and selective inhibitor of CDKs. Selective for CDK1/cyclin B kinase (IC₅₀=450nM) [2], CDK2 (IC₅₀=700nM) [4] and CDK5/p35 (IC₅₀=160nM) [4,5]. More potent than olomoucine (Prod. No. ALX-350-013). Inhibits M phase promoting factor (MPF) kinase activity. Has effects on calcium channel gating.

Product Specification

Formula:	C₁₉H₂₆N₆O

MW:	354.5

Purity:	≥97%

Appearance:	White to off-white solid.

CAS:	186692-46-6

Solubility:	Soluble in chloroform, DMSO or methanol; moderately soluble in water.

Shipping:	AMBIENT

Long Term Storage:	-20°C

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Product Literature References

Activation of cyclin-dependent kinases by Myc mediates induction of cyclin A, but not apoptosis: B. Rudolph, et al.; EMBO J. 15, 3065 (1996), Abstract;

Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5: L. Meijer, et al.; Eur. J. Biochem. 243, 527 (1997), Abstract;

Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997), Abstract;

Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997), Abstract;

Direct in vivo inhibition of the nuclear cell cycle cascade in experimental mesangial proliferative glomerulonephritis with Roscovitine, a novel cyclin-dependent kinase antagonist: J.W. Pippin, et al.; J. Clin. Invest. 100, 2512 (1997), Abstract;

Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: W.F. De Azvedo, et al.; Eur. J. Biochem. 243, 518 (1997), Abstract;

Early inhibition of DNA synthesis in the developing rat cerebral cortex by the purine analogues olomoucine and roscovitine: J.S. Yakisich, et al.; BBRC 243, 674 (1998), Abstract;

The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998), Abstract;

Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi & A. Eskin; J. Neurochem. 72, 605 (1999), Abstract;

Transcription of herpes simplex virus immediate-early and early genes is inhibited by roscovitine, an inhibitor specific for cellular cyclin- dependent kinases: L.M. Schang, et al.; J. Virol. 73, 2161 (1999), Abstract;

Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials: L. Meijer & E. Raymond; Acc. Chem. Res. 36, 417 (2003), (Review), Abstract;

The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003), Abstract;

Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004), Abstract;

Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005), Abstract;

The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction: S. Cho & S.D. Meriney; Eur. J. Neurosci. 23, 3200 (2006), Abstract;

Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007), Abstract;