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TGX-221
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TGX-221图片
CAS NO:663619-89-4
规格:98%
分子量:364.44
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
PI3Kβ inhibitor,potent,selective and ATP competitive
CAS:663619-89-4
分子式:C21H24N4O2
分子量:364.44
纯度:98%
存储:Store at -20°C

Background:

TGX-221 is a potent inhibitor of (phosphatidylinositol 3-kinases) PI3K which specifically inhibits PI3K -p110β isoform with IC50 value of 8.5 nM [1].


In J774.2 macrophage cells, TGX-221 has been demonstrated to reduce insulin-induced phosphorylation of Ser473 of protein kinase B (PKB). While in in CHO-IR and 3T3-L1 cells, TGX-221 has no effect on PKB phosphprylation [1].


In vivo, TGX-221 significantly improved blood flow in FeCl3-induced arterial thrombosis as well as increased tail and renal bleeding times in mice. In addition, TGX-221 has revealed to disrupt CFRs in a Folts model of arterial thrombosis in male Sprague-Dawley rats [2].


Reference:
[1] Chaussade C1, Rewcastle GW, Kendall JD, Denny WA, Cho K, Gr nning LM, Chong ML, Anagnostou SH,Jackson SP, Daniele N, Shepherd PR.  Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58.
[2] Bird JE1, Smith PL, Bostwick JS, Shipkova P, Schumacher WA.  Bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (PI3K)-β inhibitor in mice. Thromb Res. 2011 Jun;127(6):560-4.