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).1 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).1 Oral administration of CAY10505 reduces neutrophil recruitment in mice to an extent that is comparable to that observed in PI3Kγ-deficient mice.1
1
Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ. J Med Chem493857-3871(2006).
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Fc1ccc(cc1)c1ccc(/C=C2\SC(=O)NC/2=O)o1
Background Reading
Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ. J Med Chem493857-3871(2006).
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