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Enzastaurin is a protein kinase C beta inhibitor with 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
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