Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC). It has been shown to inhibit PKCα, βI, βII, γ, and ε with IC50 values of 8, 8, 14, 13, and 39 nM, respectively. It has also been identified as an inhibitor of Cdk2 (IC50 = 200 nM) and GSK3α/β. This compound has been used to activate mesenchymal stem cells, increase the surface expression of homing ligands that bind to intercellular adhesion molecule 1, and target delivery of these cells to sites of inflammation.
