GW406108X (Synonyms: GW108X) |
| カタログ番号GC60891 |
GW406108X は、ATPase アッセイで 0.82 uM の IC50 を持つ特異的な Kif15 (キネシン-12) 阻害剤です。強力なオートファジー阻害剤である GW406108X は、ULK1 に対する ATP 競合阻害を示し、pIC50 は 6.37 (427 nM) です。 GW406108X は、上流のシグナル伝達キナーゼ mTORC1 および AMPK に影響を与えることなく、ULK1 キナーゼ活性を阻害し、オートファジーの流れをブロックします。
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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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