双辛基马来酰亚胺是有效的，选择性的蛋白激酶C（PKC）抑制剂。它们在结构上与天然存在的分子星形孢菌素相似，但相对于其他蛋白激酶，它们对PKC的选择性更高。双辛基马来酰亚胺用于选择性探测PKC介导的激素，细胞因子和生长因子信号的转导途径。双辛基马来酰亚胺通过与催化亚基相互作用抑制PKC。抑制作用与ATP竞争。对类似物的结构-活性关系的研究表明，吲哚氮上的阳离子取代基增加了其作为PKC抑制剂的能力。 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.