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Bisindolylmaleimide III was developed as a protein kinase C (PKC) inhibitor with structural similarity to the nonspecific PKC inhibitor staurosporine. At 1 μM, bisindolylmaleimide III inhibits 93% of PKCα kinase activity and also inhibits many other protein kinases including, S6K1, MAPKAP-K1, RSK2 and MSK1 with similar potency. Additionally, it inhibits PDK1, an important kinase in the insulin signaling pathway, with an IC₅₀ value of 3.8 μM.

Bisindolylmaleimide III is a protein kinase C inhibitor and was also shown to exhibit inhibitory activities towards PDK1, an important kinase in the insulin signaling pathway,

ChEBI: Bisindolylmaleimide III is a member of maleimides and a member of indoles. It has a role as an EC 2.7.11.13 (protein kinase C) inhibitor. It is functionally related to a maleimide.