位置:首页 > 产品库 > GW806742X hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
GW806742X hydrochloride
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。
GW806742X hydrochloride图片
规格:98%
分子量:610.01
包装与价格:
包装价格(元)
5mg询价
10mg询价
25mg询价
50mg询价
100mg询价

GW806742Xhydrochloride是一种ATP模拟物,是一种有效的MLKL抑制剂,结合MLKL假激酶结构域,Kd值为9.3μM。GW806742Xhydrochloride具有抗VEGFR2的活性(IC50=2nM)。GW806742Xhydrochloride延缓MLKL膜移位并抑制坏死。
货号:ajcx31806
CAS:N/A
分子式:C25H23ClF3N7O4S
分子量:610.01
溶解度:DMSO: 100 mg/mL (163.93 mM); H2O:< 0.1 mg/mL (ultrasonic) (insoluble)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis[1][2].

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner[1].GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM[2].


[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014;111(42):15072-15077. [2]. Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523.

 
 
维奥蛋白资源库 - 中文蛋白资源 CopyRight © 2010-2024