Olomoucine

A Cyclin Dependent Kinase (CDK) Inhibitor

Product#:

O-300

Sizes:

1 mg

5 x 1 mg

5 mg

10 x 0.1 mg

Olomoucine is a cell-permeable purine protein kinase inhibitor, found to be highlyspecific for the cell-cycleregulating p34cdc2/cyclin B, p33cdk2/cyclin A and p33cdk2/cyclin E kinases,the brain p33cdk5/p35 kinase and the ERK1/2 MAP- kinase (IC₅₀=7-25 mM).¹ Olomoucinebehaves as a competitive inhibitor for ATP and as a non-competitiveinhibitor for histone H1 binding in CDKs kinases.^1-5

Olomoucine induces a dose-dependent inhibition of proliferation rate and the cell cycle progression in many human cancer cells in culture (EC₅₀=40-90mM). Olomoucine, at 1-100 mM, slowdown or arrest KB 3-1 cells in G1/S and G2/M phase and decreased the DNA synthesis of rat brain cortex.^6-11

Olomoucine also induces apoptosis in maturing cerebellar granule neurons,¹¹ NGF induced neuronal differentiationof PC12 cells in vitro¹²and in NE cells in vivo.¹³

M.W.:

298.35

CAS No.:

[1-1622-51-9]

Structure:

Purity:

>99%

Bioassay:

Olomoucine (#O-300) prevents NGF-mediated survival of PC12 cells.

PC12 cells were grown in the absence of serum. The cells were not protected (fragmented line) or protected from apoptosis with 100 ng/ml mNGF 2.5S (#N-240, continuous line) and treated with different concentrations of Olomoucine. The survival of the cells after 4 days was measured using XTT method, calculated as a relative percentage of the control without Olomoucine and plotted against Olomoucine concentrations.

References:

1.	Vesely, J. et al. (1994) Eur. J. Biochem. 224, 771.
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3.	Abraham, R.T. (1995) Biol. Cell 83, 105.
4.	Schutte, B. et al. (1997) Exp. Cell Res. 236, 4.
5.	Meijer, L. et al. (1997) Eur. J. Biochem. 243, 527.
6.	Flament, S. (2000) Zygote 8, 3.
7.	Rossi, L.A. et al. (1998) Exp. Cell. Res. 245, 8.
8.	Yakisich, J.S. et al. (1998) Biochem. Biophys. Res. Commun. 243, 674.
9.	Wesierska-Gadek, J. et al. (2004) Pol. J. Pharmacol. 56, 635.
10.	Dobashi, Y. et al. (2000) J. Biol. Chem. 275, 12572.
11.	Iseki, H. et al. (1997) Surgery 122, 187.
12.	Monaco, E.A. et al. (2004) Biochem. Pharmacol. 67, 1947.
13.	Ohnuma, S. et al. (2001) Curr. Opin. Neurobiol. 11, 66.

For research purposes only, not for human use.