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ALX-350-251 Revised 23-Oct-07
(R)-Roscovitine
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SYNONYMS 6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-251-M001   1 mg 30.00 USD Add To Cart
ALX-350-251-M005   5 mg 110.00 USD Add To Cart
ALX-350-251-M050   50 mg 450.00 USD Add To Cart
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Product Specification
FORMULA: C19H26N6O
MW: 354.5
CAS NUMBER: 186692-46-6
PURITY: ≥97%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in chloroform, DMSO or methanol; moderately soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
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 Specific Literature References
[1] 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
[2] 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
[3] 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
[4] Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997) Abstract
[5] 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
[6] 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
[7] 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
[8] 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
[9] Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi & A. Eskin; J. Neurochem. 72, 605 (1999) Abstract
[10] 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
[11] 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
[12] The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract
[13] Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) Abstract
[14] Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005) Abstract
[15] 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
[16] Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007) Abstract
Further Categories Containing This Product:
Ion Channels & Transporters Other Products
 
 

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