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(R)-Roscovitine (6-Benzylamino-2-(R)-9-isopropylpurine)

Cat no: 045188

(R)-Roscovitine (6-Benzylamino-2-(R)-9-isopropylpurine)

Potent and selective inhibitor of CDKs. More potent than olomoucine. Inhibits CDK1/cyclin B kinase (IC50 = 450 nM), CDK2 (IC50 = 700 nM) and CDK5/p35 (IC50 = 160 nM). Inhibits M phase promoting factor (MPF) kinase activity. Arrests human fibroblasts in G1 phase. Antitumor compound. Activates the mitogen-activated protein kinase pathway. Targets both the p53 and NF-kappaB pathways. Has effects on calcium channel gating. Prevents DNA damage-induced cyclin A1 upregulation. Apoptosis inducer. As CYC202 in phase I clinical trials. Reviews.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

045188

Size

1mg

Purity

>98% (NMR)

References

Product Reference: \n?Activation of cyclin-dependent kinases by Myc mediates induction of cyclin A, but not apoptosis: B. Rudolph, et al.; EMBO J. 15, 3065 (1996) \n?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) \n?Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997) \n?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) \n?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) \n?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) \n?The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003) \n?In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine): S.J. McClue, et al.; Int. J. Cancer 102, 463 (2002) \n?The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway: S.R. Whittaker, et al.; Cancer Res. 64, 262 (2004) \n?R-Roscovitine simultaneously targets both the p53 and NF-kappaB pathways and causes potentiation of apoptosis: implications in cancer therapy: A. Dey, et al.; Cell Death Differ. 15, 263 (2008) \n?The CDK inhibitor, R-roscovitine, promotes eosinophil apoptosis by down-regulation of Mcl-1: R. Duffin, et al.; FEBS Lett. 583, 2540 (2009) \n?(R)-roscovitine prolongs the mean open time of unitary N-type calcium channel currents: N.R. DeStefino, et al.; Neuroscience 167, 838 (2010) \n?R-Roscovitine (Seliciclib) prevents DNA damage-induced cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA repair: M. Federico, et al.; Mol. Cancer 9,208 (2010) \n?Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies: C. Le Tourneau, et al.; Eur. J. Cancer 46, 3243 (2010) \n?Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004) \n?Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005) \n?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) \n?Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007) \n?Cyclin-dependent kinase inhibitors as anticancer drugs: V. Krystof & S. Uldrijan; Curr. Drug Targets 11, 291 (2010) \n?Roscovitine induces cell death and morphological changes indicative of apoptosis in MDA-MB-231 breast cancer cells: O.P. Mgbonyebi, et al.; Cancer Res. 59, 1903 (1999) \n?

Alternative Names

6-Benzylamino-2-(R)--9-isopropylpurine

Read more on Supplier website

Applications

ELISA, FC, IHC, WB

Hosts

Rabbit

Reactivities

Hum

Conjugates

Biotin

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