Bisindolylmaleimides are potent, selective inhibitors of protein kinase C (PKC). They are structurally similar to the naturally occurring molecule, staurosporine, but they are more selective for PKC over other protein kinases. Bisindolylmaleimides are used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. Bisindolylmaleimides inhibit PKC by interacting with the catalytic subunit. Inhibition is competitive with ATP. Studies of structure-activity relationships of analogs indicate that cationic substituents at the indole nitrogen increase the potency as an inhibitor of PKC.
