Enzastaurin is a potent inhibitor of PKCβ (IC50 = 6 nM), with modest selectivity over PKCα, PKCγ, and PKCε (IC50 = 39, 83, and 110 nM, respectively). At 3 μM, enzastaurin also inhibits signaling through the Akt pathway. It suppresses angiogenesis, induces apoptosis, and reduces proliferation of cultured tumor cells. Because of these effects, enzastaurin has potential antineoplastic activity.
