GW406108X (Synonyms: GW108X)
目录号: PL12506 纯度: ≥98.0%
CAS No. :1644443-92-4
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中文名称
GW406108X
英文名称
GW406108X
英文别名
GW406108X;GW108X;HMS3303K19;HMS3306L01;BDBM50085411;NSC756222;3-(3,5-Dichloro-4-hydroxybenzylidene)-5-(2-furanylcarbonyl)indoline-2-one;(Z)-3-(3,5-Dichloro-4-hydroxybenzylidene)-5-(furan-2-carbonyl)indolin-2-one;3-[1-(3,5-Dichloro-4-hydroxy-phenyl)-meth-(Z)-ylidene]-5-(furan-2-carbonyl)-1,3-dihydro-indol-2-one
Cas No.
1644443-92-4
分子式
C20H11Cl2NO4
分子量
400.21
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GW406108X 是特异性的 Kif15 (Kinesin-12) 抑制剂,IC50 为 0.82 uM。GW406108X 是一种有效的自噬 (autophagy) 抑制剂, ATP 竞争性抑制 ULK1,pIC50 为 6.37 (427 nM)。GW406108X 抑制 ULK1 和自噬,而不影响 mTOR 或 AMPK 活性。
生物活性
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC 50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC 50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
性状
Solid
体外研究(In Vitro)
GW406108X acts upon ULK1 and autophagy without affecting mTOR or AMPK activity as shown by monitoring ULK1 pS758 (mTOR site) or pS556 (AMPK site) levels. GW406108X inhibits VPS34 and AMPK with pIC50 of 6.34 (457 nM) and 6.38 (417 nM), respectively. In the presence of 5 μΜ GW406108X, the starvation-induced increase in ATG13 phosphorylation is significantly reduced.
GW406108X inhibits Kif15-N420 ATPase activity by 76%. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Zachari M, et al. The identification and characterisation of autophagy inhibitors from the published kinase inhibitor sets. Biochem J. 2020;477(4):801-814.
[2]. Dumas ME, et al. Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. Bioorg Med Chem Lett. 2019;29(2):148-154.
溶解度数据
In Vitro: DMSO : 50 mg/mL (124.93 mM; Need ultrasonic)配制储备液
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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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