Cas No.: | 1808714-73-9 |
Chemical Name: | N-[4-fluoro-3-(prop-2-enamido)phenyl]-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide |
Synonyms: | EN6 |
SMILES: | FC1C=CC(NC(C2C=NN(C3C=CC=CC=3F)C=2)=O)=CC=1NC(=O)C=C |
Formula: | C19N4O2F2H14 |
M.Wt: | 368.3369 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase). 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[1]. |
References: | [1]. Chung CY, et al. Covalent targeting of the vacuolar H+-ATPase activates autophagy via mTORC1 inhibition. Nat Chem Biol. 2019 Aug;15(8):776-785. |