Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.

PKCβ2:163 nM, PKCγ:213 nM, PKC:158 nM(Rat Brain), PKCβ1:195 nM, PKCε:175 nM, PKCα:53 nM

Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases. Bisindolylmaleimide VIII acetate (5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners. Bisindolylmaleimide VIII acetate (5 μM; 6 hours) significantly decreases procaspase-8 at 4 h and completely disappears at 6 h after the combined treatment with TRA-8 [2].

Bisindolylmaleimide VIII acetate (100 μg; i.p.; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. The alone treatment with Bisindolylmaleimide VIII acetate does not induce significant tumor regression [2].