5-喹喔啉-6-亚甲基-1，3-噻唑烷-2，4-二酮（AS 605240）是一种PI 3-κ B的ATP竞争性抑制剂（IC 50 = 8 nM）。它对β 3-同种型具有选择性（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浓度下对多种蛋白激酶无显著活性。此外，AS 605240还可抑制类风湿性关节炎小鼠模型中关节炎症的进展，并抑制狼疮小鼠模型中的炎症。参考文献Powered by Bioz查看更多详情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抑制阻断肾小球肾炎并延长系统性狼疮小鼠模型的寿命”Nature Medicine 2005 11 933-935。
产品描述
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 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.
