Olomoucine

Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 µM), CDK/p35 kinase (IC50=3 µM) and ERK1/p44 MAP kinase (IC50=25 µM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.

Cancer-Kinase/protease

[1].Hajdúch M, et al. Induction of apoptosis and regression of spontaneous dog melanoma following in vivo application of synthetic cyclin-dependent kinase inhibitor olomoucine. Anticancer Drugs. 1997 Nov. 8(10):1007-13. | [2].Raynaud FI, et al. Cassette dosing pharmacokinetics of a library of 2, 6, 9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis. Mol Cancer Ther. 2004 Mar. 3(3):353-62. | [3].Vesely, J., Havlicek, J., Strnad, M., et al. Inhibition of cyclin-dependent kinases by purine analogues. European Journal of Biochemistry 224, 771-786 (1994). | [4].Abraham, R.T., Acquarone, M., Andersen, A., et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biology of the Cell 83(2), 105-120 (1995).

Others

CDK

Cell Cycle/DNA Damage