Enzastaurin (Enz) is a potent and selective inhibitor of PKC with antiproliferative activity (IC= ~6 nM). Binding to the ATP-, enzastaurin selectively inhibits Protein kinase & protein kinase C beta. Enz suprpresses VEGF-induced angiogenesis in the rat corneal micropocket assay, decreases microvessel density, and prevents VEGF secretion from human tumor cell xenografts in nude mice. Prolonged courses of Enz increase chemotherapy or radiation tumor growth delay of glioma, breast, and small cell lung cancer xenografts.
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