Lieferant:
ENZO LIFE SCIENCES
Beschreibung:
Olomoucine is a purine derivative which acts as a potent and selective inhibitor of CDK1 (p34cdc2)/cyclin B and related kinases. It acts by competing for the ATP binding domain of the kinase. Of 35 protein kinases tested, Olomoucine inhibited p33CDK2/cyclin A, p33CDK2/cyclin E, p34cdc2/cyclin B, p33CDK5/p35 and erk1 with IC50 of 7, 7, 7, 3 and 25µM respectively. The related kinases p34CDK4/cyclin D and p40CDK6/cyclin D3 were not inhibited or were less sensitive to Olomoucine, IC50 > 1000 and 250µM respectively. PKC, PKA, PKG, CaM kinase II, MLC kinase, CK2, EGFR tyrosine kinase, p56lck, p56lyn, p60c-src, v-abl and insulin receptor tyrosine kinase are not inhibited or are weakly inhibited at 1mM. It delays mouse oocyte maturation and inhibits the growth of a variety of human cell lines including Rhabdomyosarcoma cell line Rh1, Rh18, Rh28 and Rh30; MCF-7, KB-3-1 and their adriamycin-resistant counterparts (IC50=18-86µM). It inhibits DNA synthesis in interleukin-2-stimulated T lymphocytes and triggers a G1 arrest similar to interleukin-2 deprivation. Can be used to synchronize cells in G1. Triggers apoptosis in target tumor cells in vitro and in vivo and in maturing cerebellar granule neurons. N9-Isopropyl-Olomoucine and the negative control Iso-Olomoucine are also available.
