5-喹喔啉-6-亞甲基-1，3-噻唑烷-2，4-二酮（AS 605240）是一種PI 3-κ B的ATP競爭性抑制劑（IC 50 = 8 nM）。它對β 3-同種型具有選擇性（IC 50：PI 3-κ 2 ± = 60 nM PI 3-κ 2 2 = 270 nM PI 3-κ 2 ′ = 300 nM），在1 μ M濃度下對多種蛋白激酶無顯著活性。此外，AS 605240還可抑制類風濕性關節炎小鼠模型中關節炎癥的進展，并抑制狼瘡小鼠模型中的炎癥。參考文獻Powered by Bioz查看更多詳情Bioz 1）M. Camps等人“Blockade of PI3Kg suppresses joint inflammation and damage in mouse models of rheumatoid arthritis”Nature Medicine 2005 11 936-943.2）D.F. Barber等人，“PI 3 Kg抑制阻斷腎小球腎炎并延長系統性狼瘡小鼠模型的壽命”Nature Medicine 2005 11 933-935。
產品描述
5-quinoxilin-6-methylene-1 3-thiazolidine-2 4-dione (AS605240) is an ATP-competitive inhibitor of PI3-K?3 (IC50 = 8 nM). It is selective for the ?3-isoform (IC50: PI 3-K?± = 60 nM PI 3-K?2 = 270 nM PI 3-K?′ = 300 nM) and shows no notable activity against a wide array of protein kinases at 1 ??M. 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 Bioz See more details on 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.
