GW 806742X

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子 MLKL（混合谱系激酶结构域）相互作用因子，可结合 MLKL 假激酶结构域 (Kd=9.3 uM)。

A small molecule MLKL (Mixed Lineage Kinase Domain-Like) interactor that binds the MLKL pseudokinase domain (Kd=9.3 uM), retards membrane association to inhibit necroptosis; rescues 50% of wild-type MDFs from TSQ-induced necroptosis with IC50 <50 nM, with >50-fold greater potency than Nec-1; enhances RIPK3-mediated phosphorylation of MLKL (S345 and S347) at 10 uM.

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.?GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM.

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GW806742X

MAPK/ERK Signaling

MLK

MLK

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579515-63-2

573.551

C25H22F3N7O4S

>98% (HPLC)

DMSO : ≥ 125 mg/mL 217.94 mM

CN(C1=CC=C(C=C1)NC(=O)NC2=CC=C(C=C2)OC(F)(F)F)C3=NC(=NC=C3)NC4=CC(=CC=C4)S(=O)(=O)N

3-((4-(methyl(4-(3-(4-(trifluoromethoxy)phenyl)ureido)phenyl)amino)pyrimidin-2-yl)amino)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years