EN6

EN6 is an activator of autophagy. It inhibits mammalian target of rapamycin complex 1 (mTORC1) signaling by binding covalently to cysteine 277 of the ATP6V1A catalytic subunit of the lysosomal vacuolar ATPase (v-ATPase) and impairing v-ATPase coupling with Rag GTPases. It is selective for inhibition of mTORC1 over mTORC2 signaling. EN6 increases lysosome acidification and increases cellular clearance of TDP-43 protein aggregates, which are a pathological feature of several neurodegenerative diseases, in a v-ATPase-dependent manner in U2OS osteosarcoma cells. It also inhibits mTORC1 signaling and enhances autophagy in mouse skeletal muscle and heart when administered at a dose of 50 mg/kg.Formal Name: N-[4-fluoro-3-[(1-oxo-2-propen-1-yl)amino]phenyl]-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide. CAS Number: 1808714-73-9. Molecular Formula: C19H14F2N4O2. Formula Weight: 368.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:10): 0.09 mg/ml, DMSO: 15 mg/ml. lambdamax: 268 nm. SMILES: FC1=C(NC(C=C)=O)C=C(NC(C2=CN(C3=C(F)C=CC=C3)N=C2)=O)C=C1. InChi Code: InChI=1S/C19H14F2N4O2/c1-2-18(26)24-16-9-13(7-8-14(16)20)23-19(27)12-10-22-25(11-12)17-6-4-3-5-15(17)21/h2-11H,1H2,(H,23,27)(H,24,26). InChi Key: SUSXQEYPNDORDQ-UHFFFAOYSA-N.