General description

A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3β, JAK3, PKCα and PKCθ (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 µM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC₅₀ = 0.525, 1.294 and 0.689 µM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Haan, C., et al. 2011. Chem. Biol.18, 314.Thoma, G., et al. 2011. J. Med. Chem.54, 284.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)