PKC-412, a staurosporine derivative, has been shown to possess antiproliferative characteristics via inhibition of PKC (protein kinase C), Flk (kinase insert domain receptor), and c-kit. This compound has been shown to cause an increase in the G2/M phase of the cell cycle related to polyploidy, enhanced sensitivity to ionizing radiation, and apoptosis. Additionally, PKC-412 has been reported to inhibit Flt-3/Flk-2 tyrosine kinase which consequentially causes induced G1 arrest and apoptosis of Ba/F3 cell lines. Other experiments have noted that this agent demonstrates the ability to increase endothelial nitric oxide (NO) synthase expression and NO production in cultured human endothelial cells. PKC-412 is an inhibitor of c-Src, Cdk1, cyclin B, EGFR, Flk-1, Flt-1, PDGFR-β, PKA, PKC α, PKC β, PKC γ, PKC δ, PKC η, Fgr and Syk.
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See how others have used PKC-412 (CAS 120685-11-2). Click on the entry to view the PubMed entry .
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