GW806742X hydrochloride
目录号: PL07384 纯度: ≥98%
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中文名称
GW806742X hydrochloride
英文名称
GW806742X hydrochloride
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
GW806742X hydrochloride 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 9.3 μM。GW806742X hydrochloride 具有抗 VEGFR2 的活性 (IC50=2 nM)。GW806742X hydrochloride 延缓 MLKL 膜移位并抑制坏死。
生物活性
GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K d of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC 50 =2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
性状
Solid
IC50 & Target[1][2]
MLKL 9.3 μM (Kd) VEGFR2 2 nM (IC50)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (163.93 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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