PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM. It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice. PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.
