A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3b, JAK3, PKCa and PKCth (IC50=3, 8, 13 and 68nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50=1.017, 2.55 and 8.055uM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50=0.525, 1.294 and 0.689uM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).
Synonyms: 3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione, NIBR3049, JAK3 Inhibitor XII
Molecular Formula:C₂₇H₂₅F₃N₄O₄
Molecular Weight:526.5
Solubility:DMSO
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.