5-quinoxilin-6-methylene-1,3-thiazolidine-2,4-dione (AS605240) is an ATP-competitive inhibitor of PI3-Kγ (IC50 = 8 nM). It is selective for the γ-isoform (IC50: PI 3-Kα = 60 nM, PI 3-Kβ = 270 nM, PI 3-Kδ = 300 nM) and shows no notable activity against a wide array of protein kinases at 1 μM. In addition, AS605240 suppresses the progression of joint inflammation in a mouse model of rheumatoid arthritis and suppresses inflammation in a mouse model of lupus.
References
Powered by Bioz1) M. Camps et al. “Blockade of PI3Kg suppresses joint inflammation and damage in mouse models of rheumatoid arthritis” Nature Medicine, 2005, 11, 936-943.
2) D.F. Barber, et al., “PI3Kg inhibition blocks glomerulonephritis and extends lifespan in a mouse model of systemic lupus” Nature Medicine, 2005, 11, 933-935.
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