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CAS No.: 579515-63-2

GW806742X Catalog No. CSN27743

Synonyms: GW806742X

GW806742X is an ATP mimetic MLKL inhibitor with Kd value of 9.3μM, and a VEGFR2 inhibitor with IC50 value of 2nM.

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技术信息

生物活性

描述Mixed lineage kinase domain-like (MLKL) is the terminal protein in the pro-inflammatory necroptotic cell death program. RIPK3-mediated phosphorylation is thought to initiate MLKL oligomerization, membrane translocation and membrane disruption^[3]. MLKL promotes vascular inflammation by regulating the expression of adhesion molecules ICAM1, VCAM1, and E-selectin in endothelial cells (EC). MLKL deficiency suppresses the expression of these adhesion molecules, thereby reducing EC-leukocyte interaction in vitro and in vivo^[4]. MLKL-induced membrane depolarization and cell death exhibit a positive correlation to its channel activity. The Mg(2+)-preferred permeability and five transmembrane segment topology distinguish MLKL from previously identified Mg(2+)-permeable channels and thus establish MLKL as a novel class of cation channels^[5].Mice deficient in MLKL (Mlkl-/-) had reduced neuronal death (24 h) and BBB permeability at 24 h but not 30d, and improved post-injury rotarod performance vs. WT^[6]. MLKL activation is sufficient to induce the processing and release of bioactive IL-1β. MLKL activation triggers potassium efflux and assembly of the NLRP3 inflammasome, which is required for the processing and activity of IL-1β released during necroptosis. Notably, MLKL activation also causes cell membrane disruption, which allows efficient release of IL-1β independently of the recently described pyroptotic effector gasdermin-D^[7]. GW806742X, an ATP mimetic and a potent MLKL inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis^[8].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7435 mL
- 8.7177 mL
- 17.4354 mL
- 5 mM
- 0.3487 mL
- 1.7435 mL
- 3.4871 mL
- 10 mM
- 0.1744 mL
- 0.8718 mL
- 1.7435 mL

技术信息

CAS号

579515-63-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H22F3N7O4S

运输

蓝冰

分子量

573.55

别名

GW806742X

溶解度

DMSO	125.0 mg/mL (217.9 mM)

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