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EN6

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Chemical Structure| 1808714-73-9 同义名 : -
CAS号 : 1808714-73-9
货号 : A1060682
分子式 : C19H14F2N4O2
纯度 : 99%+
分子量 : 368.337
MDL号 : MFCD31665468
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 4 mg/mL(10.86 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 1 mg/mL(2.71 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 The vacuolar H+-ATPase (v-ATPase) is a universal component of eukaryotic organisms, which is present in both intracellular compartments and the plasma membrane. Its proton-pumping action creates the low intravacuolar pH, benefiting many processes such as, membrane trafficking, protein degradation, renal acidification, bone resorption, and tumor metastasis [1]. EN6 is a small-molecule activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase, which activates mechanistic target of rapamycin complex 1 (mTORC1) via the Rag guanosine triphosphatases. EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner [2].
作用机制 EN6 covalently binds to cysteine 277 in the ATP6V1A subunit of v-ATPase .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.15mL

5.43mL

2.71mL

参考文献

[1]Xiao YT, Xiang LX, Shao JZ. Vacuolar H(+)-ATPase. Int J Biochem Cell Biol. 2008;40(10):2002-6. doi: 10.1016/j.biocel.2007.08.006. Epub 2007 Aug 22. PMID: 17897871.

[2]Chung CY, Shin HR, Berdan CA, Ford B, Ward CC, Olzmann JA, Zoncu R, Nomura DK. Covalent targeting of the vacuolar H+-ATPase activates autophagy via mTORC1 inhibition. Nat Chem Biol. 2019 Aug;15(8):776-785. doi: 10.1038/s41589-019-0308-4. Epub 2019 Jul 8. PMID: 31285595; PMCID: PMC6641988.