GW406108X (Synonyms: GW108X) |
| Catalog No.GC60891 |
GW406108X est un inhibiteur spécifique de Kif15 (kinésine-12) avec une IC50 de 0,82 uM dans les dosages ATPase. GW406108X, un puissant inhibiteur de l'autophagie, montre une inhibition compétitive de l'ATP contre ULK1 avec un pIC50 de 6,37 (427 nM). GW406108X inhibe l'activité de la kinase ULK1 et bloque le flux autophagique, sans affecter les kinases de signalisation en amont mTORC1 et 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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