Chemical Structure : Autophagy activator EN6
CAS No.: 1808714-73-9
Catalog No.: PC-72988Not For Human Use, Lab Use Only.
Autophagy activator EN6 (EN6) is a small-molecule in vivo activator of autophagy, covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase (vacuolar H+-ATPase).
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Autophagy activator EN6 (EN6) is a small-molecule in vivo activator of autophagy, covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase (vacuolar H+-ATPase).
The lysosomal v-ATPase (vacuolar H+-ATPase) activates mTORC1 via the Rag guanosine triphosphatases.
EN6 displaced tetramethylrhodamine-5-iodoacetamide dihydroiodide (IA-rhodamine) labeling from recombinant human ATP6V1A protein with IC50 of 1.7 uM.
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.
M.Wt | 368.344 | |
Formula | C19H14F2N4O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(3-acrylamido-4-fluorophenyl)-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide |
1. Chung CY, et al. Nat Chem Biol. 2019 Jul 8. doi: 10.1038/s41589-019-0308-4.
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