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GW406108X
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GW406108X图片
CAS NO:1644443-92-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
GW406108X是特异性的Kif15(Kinesin-12)抑制剂,IC50为0.82uM。GW406108X是一种有效的自噬(autophagy)抑制剂,ATP竞争性抑制ULK1,pIC50为6.37(427nM)。GW406108X抑制ULK1和自噬,而不影响mTOR或AMPK活性。
Cas No.1644443-92-4
别名GW108X
Canonical SMILESO=C1NC2=C(C=C(C(C3=CC=CO3)=O)C=C2)/C1=C/C4=CC(Cl)=C(O)C(Cl)=C4
分子式C20H11Cl2NO4
分子量400.21
溶解度DMSO: 62.5 mg/mL (156.17 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signalling kinases mTORC1 and AMPK[1][2].

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[1].GW406108X inhibits Kif15-N420 ATPase activity by 76%[2].

[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.