GW406108X (Synonyms: GW108X) |
| رقم الكتالوجGC60891 |
GW406108X هو مثبط Kif15 (Kinesin-12) محدد مع IC50 يبلغ 0.82 ميكرومتر في فحوصات ATPaseيُظهر GW406108X ، مثبط الالتهام الذاتي القوي ، تثبيط ATP التنافسي ضد ULK1 مع pIC50 من 6.37 (427 نانومتر)GW406108X يثبط نشاط كيناز ULK1 ويمنع التدفق الذاتي ، دون التأثير على كينازات الإشارات المنبع mTORC1 و AMPK
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Cas No.: 1644443-92-4
Sample solution is provided at 25 µL, 10mM.
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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.
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