产品描述:
Phosphoinositide 3-kinase γ (PI3Kγ), expressed primarily in hematopoietic cells, plays several important roles in immunity. 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).{14230} 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 mouse macrophages (IC50 = 228 nM).{14230} Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.{14230}