Enzastaurin (LY317615) is a potent, selective, ATP-competitive PKCβ inhibitor with IC50 of 6 nM.
Enzastaurin (LY317615) weakly inhibits PKCα, PKCγ, and PKCε with IC50 of 39, 83, and 110 nM, respectively.
Enzastaurin (LY317615) induces apoptosis and suppresses the proliferation of tumor cells, suppresses the phosphorylation of GSK3β Ser9, ribosomal protein S6(S240/244) and AKT(Thr308).
Enzastaurin (LY317615) suppresses tumor growth through multiple mechanism in vivo; orally active.
