1808714-73-9
Chemical Structure
EN6
- CAS No.: 1808714-73-9
- Formula:C19H14F2N4O2
- Molecular Weight:368.34
IUPAC Name: N-(3-acrylamido-4-fluorophenyl)-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide
InChIKey: SUSXQEYPNDORDQ-UHFFFAOYSA-N
SMILES: O=C(C1=CN(C2=CC=CC=C2F)N=C1)NC3=CC=C(F)C(NC(C=C)=O)=C3
Biological Activity: EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner[1].
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EN6 | 99.32% | EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner. | ||||||||||||||||||||
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