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  • GW806742X hydrochloride
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GW806742X hydrochloride

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。

原价
¥650-4850
价格
520-3880
GW806742X hydrochloride的二维码

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  • 库存: 现货
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  • 货号: ajcx31806
  • CAS: N/A
  • 别名:
  • 分子式: C25H23ClF3N7O4S
  • 分子量: 610.01
  • 纯度: >98%
  • 溶解度: DMSO: 100 mg/mL (163.93 mM); Water: < 0.1 mg/mL (ultrasonic) (insoluble)
  • 储存: 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.

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