Bisindolylmaleimide VIII

Bisindolylmaleimide VIII is a selective PKC (protein kinase C) inhibitor, with observed binding activity to dystrophia myotonica protein kinase (DMPK). Bisindolylmaleimide VIII is suggested as being slightly more specific for PKC α over PKC β, PKC γ, and PKC ε isozymes (IC₅₀ = 53, 195, 213, and 275 respectively). The compound has been shown to improve DR5-mediated apoptosis through the MKK4/JNK/p38 kinase. When bisindolylmaleimide VIII is combined with TRA-8 it can activate c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase. Studies have shown that bisindolylmaleimide VIII enhance Fas-mediated apoptosis in both human astrocytoma 1321N1 cells and in Molt-4T cells.