Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Olomoucine is a cdk inhibitor that acts by competing for the ATP binding site of the kinase. This purine derivative is an inhibitor for CDC2/cyclin B (IC50 = 7 µM), CDK2/cyclin A (IC50 = 7 µM), CDK2/cyclin E (IC50 = 7 µM), CDK/p35 kinase (IC50 = 3 µM), and ERK1/p44 MAP kinase (IC50 = 25 µM).1 Olomoucine inhibits DNA synthesis in interleukin-2 stimulated T lymphocytes, triggers G1 arrest, and is also used to synchronize cells in G1.2 This inhibitor can attenuate astroglial proliferation and glial scar formation, decrease lesion cavity and mitigate functional deficits after spinal cord injury (SCI) in rats.3 Administration of olomoucine (3 mg/kg/day) to rats after SCI significantly suppressed microglial proliferation and proinflammatory cytokine expression, reduced tissue edema formation, and attenuated the number of apoptotic neurons.3
1
Veselý, J., Havlicek, J., Strnad, M., et al. Inhibition of cyclin-dependent kinases by purine analogues. Eur J Biochem224771-786(1994).
2
Abraham, R.T., Acquarone, M., Andersen, A., et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biol Cell83(2)105-120(1995).
3
Tian, D., Xie, M., Yu, Z., et al. Cell cycle inhibition attenuates microglia induced inflammatory response and alleviates neuronal cell death after spinal cord injury in rats. Brain Res1135177-185(2007).
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SMILES
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OCCNc1nc(NCc2ccccc2)c2ncn(C)c2n1
Background Reading
Abraham, R.T., Acquarone, M., Andersen, A., et al. Cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. Biol Cell83(2)105-120(1995).
Tian, D., Xie, M., Yu, Z., et al. Cell cycle inhibition attenuates microglia induced inflammatory response and alleviates neuronal cell death after spinal cord injury in rats. Brain Res1135177-185(2007).
Olomoucine is available in the following screening
libraries: