5-[[5-(4-Fluorophenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione

DescriptionPhosphoinositide 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

UsesPOSH-IN-1 (Compound 108) is an inhibitor for POSH polypeptide, that inhibits the ubiquitin ligase of POSH with an IC50 of 900 nM[1].