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Roscovitine, 5 mg  

Roscovitine, 5 mg

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

Synonyms: CYC202
potent and selective CDK (CDK1, CDK2, CDK5) inhibitor

More details

PKI-RSCV-005

Availability: within 3 days

300,00 €

Background: Roscovitine is a potent and selective inhibitor of cyclin-dependent protein kinases (CDKs). It is selective forCDK1/ CycB (IC50 = 0.65 µM), CDK2/CycA (IC50 = 0.7 µM), CDK2/CycE (IC50 = 0.7 µM), CDK3/CycE (IC50 =1.4 µM), CDK5/p25 (IC50 = 0.2 µM), CDK7/CycH (IC50 =0.5 µM), CDK9/CycT1 (IC50 =0.6 µM), but not for CDK4 or CDK6 (IC50 >100µM). The compound inhibits the proliferation of mammalian cell lines with an average IC50 of 16 µM and inhibits M phase promoting factor (MPF) kinase activity. Furthermore, PDXK was identified as a (R)-roscovitine-binding protein. Crystal structure analysis revealed, that interaction occurs with the pyridoxal – binding site rather than the ATP – binding site of PDXK. The effects of (R)-roscovitine on the catalytic activity of PDXK are rather limited.

Chemical formula: C19H26N6O
Molecular weight: 354.5 g/mol
Purity: > 97%
Appearance: White powder
Solubility: Soluble in chloroform, DMSO or methanol; moderately soluble in water
CAS Number: 186692-46-6

Also available predissolved at 10 mM in our CDK Inhibitor Set.

Product specific literature references:

De Azevedo WF, Leclerc S, Kim SH et al. (1997) "Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine" Eur J Biochem. 15;243 (1-2):518-26

Meijer L, Borgne A, Moulinoux JP et al. (1997) "Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5" Eur J Biochem. 15;243 (1-2):527-36

Planchais S, Glab N, Bergounioux C et al. (1997) "Roscovitine, a novel cyclin-dependent kinase inhibitor, characterizes restriction point and G2/M transition in tobacco BY-2 cell suspension" Plant J. 12(1):191-202

Alessi F, Quarta S, Prosperi E (1998) "The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity" Exp Cell Res. 245(1):8-18

Mgbonyebi OP, Russo J, Russo IH (1999) "Roscovitine induces cell death and morphological changes indicative of apoptosis in MDA-MB-231 breast cancer cells" Cancer Res. 59(8):1903-10

Edamatsu H, Gau CL, Nemoto T, Guo L, Tamanoi F (2000) "Cdk inhibitors, roscovitine and olomoucine, synergize with farnesyltransferase inhibitor (FTI) to induce efficient apoptosis of human cancer cell lines" Oncogene 19(27):3059-68

Schang LM, Rosenberg A, Schaffer PA (2000) "Roscovitine, a specific inhibitor of cellular cyclin-dependent kinases, inhibits herpes simplex virus DNA synthesis in the presence of viral early proteins" J Virol. 74(5):2107-20

Ljungman M, Paulsen MT (2001) "The cyclin-dependent kinase inhibitor roscovitine inhibits RNA synthesis and triggers nuclear accumulation of p53 that is unmodified at Ser15 and Lys382" Mol Pharmacol. 60(4):785-9

McClue SJ, Blake D, Lane DP et al. (2002) "In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine)" Int J Cancer 102(5):463-8

Mohapatra S, Chu B, Pledger WJ et al. (2003) "Roscovitine inhibits STAT5 activity and induces apoptosis in the human leukemia virus type 1-transformed cell line MT-2" Cancer Res. 63(23):8523-30

Whittaker SR, Walton MI, Garrett MD, Workman P (2004) "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" Cancer Res. 64(1):262-72

Tirado OM, Mateo-Lozano S, Notario V (2005) "Roscovitine is an effective inducer of apoptosis of Ewing\'s sarcoma family tumor cells in vitro and in vivo" Cancer Res. 65(20):9320-7

Crescenzi E, Palumbo G, Brady HJ (2005) "Roscovitine modulates DNA repair and senescence: implications for combination chemotherapy" Clin Cancer Res. 11(22):8158-71

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

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