AS605240 (PI3-K gamma Inhibitor 1)

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

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1) 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.