Description:CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the γ isoform (IC50 = 30 nM) better than the α, β, and δ isoforms (IC50 = 0.94, 20, and 20 μM, respectively). Tested against a panel of 80 other kinases, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK2, IC50 = 20 nM). It also inhibits the phosphorylation of the PI3K substrate PKB/Akt in murine macrophages (IC50 = 228 nM). Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.
Formulation:A crystalline solid
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