Olomoucine. A Cyclin Dependent Kinase (CDK) Inhibitor.
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 uM).
Olomoucine�behaves as a competitive inhibitor for ATP and as a non-competitive�inhibitor for histone H1 binding in CDKs kinases.
Olomoucine induces a dose-dependent inhibition�of proliferation rate�and the cell cycle progression in many human cancer cells in culture (EC50=40-90uM). Olomoucine, at 1-100 uM, slowdown or arrest KB 3-1 cells in G1/S and G2/M phase and decreased the DNA synthesis of rat brain cortex.
Olomoucine also induces apoptosis in maturing cerebellar granule neurons,�NGF induced neuronal differentiation�of PC12 cells�in�vitro�and in NE cells�in�vivo.
Protein Kinase Inhibitors and Activators; CDK Inhibitors
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