|N-[4-氟-3-(丙-2-烯酰胺基）苯基]-1-(2-氟苯基)-1H-吡唑-4-甲酰胺|CsnPharm

CAS No.: 1808714-73-9

EN6 Catalog No. CSN24507

EN6 covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase). It is a small-molecule in vivo activator of autophagy.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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 .
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7149 mL
- 13.5745 mL
- 27.1491 mL
- 5 mM
- 0.5430 mL
- 2.7149 mL
- 5.4298 mL
- 10 mM
- 0.2715 mL
- 1.3575 mL
- 2.7149 mL

技术信息

CAS号

1808714-73-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H14F2N4O2

运输

蓝冰

分子量

368.34

别名

溶解度

DMSO	160.0 mg/mL (434.4 mM)
Water	insoluble

动物实验配方

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EN6 Catalog No. CSN24507

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