K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c.
Chin LS, Murray SF, Doherty PF, Singh SK.
Department of Neurosurgery, University of Maryland School of Medicine,
Baltimore, USA. lchin@surgery1.umaryland.edu
The indole carbazole K252a has been shown in previous studies to inhibit the
platelet-derived growth factor signal transduction pathway in gliomas. Because
K252a has nonspecific effects on protein kinase function, we studied its effect
on cyclin-dependent kinases (CDK) and cell cycle blockade in glioma cells. K252a
blocked T98G cells at the G1/S and G2/M checkpoints. Consistent with cell cycle
arrest, K252a was shown to hypophosphorylate Rb, upregulate p21, and decrease
Cdc2 and Cdc25c activity. Finally, cell cycle arrest in T98G cells resulted in
apoptosis as determined by cell morphology and DNA laddering. K252a is a useful
tool for studying the effects of CDK inhibition and cell cycle blockade in tumor
cells.
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