Overview
- Veseley, J. et al. (1994) Eur. J. Biochem. 224, 771.
- Monaco, E.A. et al. (2004) Biochem. Pharmacol. 67, 1947.
- Alomone Labs Olomoucine prevents NGF-mediated survival of PC-12 cells.Cells were grown in the absence of serum. The cells were not protected (dotted line) or protected (continuous line) from apoptosis with 100 ng/ml Native mouse NGF 2.5S protein (99%) (#N-240) and treated with different concentrations of Olomoucine (#O-300). Cell survival was measured after 4 days using the XTT method, calculated as a relative percentage of the control without Olomoucine and plotted against Olomoucine concentrations.
Olomoucine is a cell-permeable purine protein kinase inhibitor, found to be highly specific for the cell-cycle regulating 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 µM).1 Olomoucine behaves as a competitive inhibitor for ATP and as a non-competitive inhibitor 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 = 40-90 µM). Olomoucine, at 1-100 µM, 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 differentiation of PC12 cells in vitro12 and in NE cells in vivo.13