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GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).1 It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.
WARNING This product is not for human or veterinary use.
1. Optimization of novel indazoles as highly potent and selective inhibitors of phosphoinositide 3-