CAY10505

Description

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

References

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. Chem. 49(13),3857-3871(2006).