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Description

A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3beta, JAK3, PKCalpha and PKCtheta (IC50 = 3, 8, 13 and 68 nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50 = 1.017, 2.55 and 8.055 µ,M, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50 = 0.525, 1.294 and 0.689 µ,M in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).