Olomoucine, 5 mg

Background: Olomoucine is a cyclin-dependent kinase inhibitor that competes for the ATP binding site of the kinase. It selectively inhibits cdc2/cyclin B (IC50 = 7 µM), cdk2/cyclin A (IC50 = 7 µM), cdk2/cyclin E (IC50 = 7 µM), cdk5/p35 kinase (IC50 = 3 µM) and  p44 ERK1/MAP kinase (IC50 = 25 µM). It exhibits reduced sensitivity towards related kinases such as cdk4/cyclin D (IC50 > 1 mM) and cdk6/cyclin D3 (IC50 > 250 µM) and does not significantly affect the activity of other protein kinases at 1 mM. It arrests human fibroblasts in the G1 phase and is known to inhibit DNA synthesis in interleukin-2-stimulated T lymphocytes.

Chemical formula: C15H18N6O
Molecular weight: 298.4 g/mol
Purity: >98%
Appearance: White solid
Solubility: soluble in ethanol
CAS number: 101622-51-9

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

Product specific literature references:

Glab N, Labidi B, Qin LX, Trehin C, Bergounioux C, Meijer L (1994) "Olomoucine, an inhibitor of the cdc2/cdk2 kinases activity, blocks plant cells at the G1 to S and G2 to M cell cycle transitions" FEBS Lett. 1994 Oct 17;353(2):207-11

Abraham RT, Acquarone M, Andersen A, Asensi A, Belle R, Berger F, Bergounioux C, Brunn G, Buquet-Fagot C, Fagot D, et al. (1995) "Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases" Biol. Cell. 83(2-3):105-20

Havlicek L, Hanus J, Vesely J, Leclerc S, Meijer L, Shaw G, Strnad M (1997) "Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds" J. Med. Chem. 40(4):408-12

Alessi F, Quarta S, Savio M, Riva F, Rossi L, Stivala LA, Scovassi AI, Meijer L, 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

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

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