An activator of autophagy; inhibits mTORC1 signaling by covalently binding to the lysosomal v-ATPase; selective for inhibition of mTORC1 over mTORC2 signaling; increases lysosome acidification and increases cellular clearance of TDP-43 protein aggregates in a v-ATPase-dependent manner in U2OS osteosarcoma cells; inhibits mTORC1 signaling and enhances autophagy in mouse skeletal muscle and heart at 50 mg/kg

EN6 – 10 mg

Brand:
Cayman
CAS:
1808714-73-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

EN6 is an activator of autophagy.{50201} 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.  

 

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SKU: 28715 - 10 mg Category:

Description

An activator of autophagy; inhibits mTORC1 signaling by covalently binding to the lysosomal v-ATPase; selective for inhibition of mTORC1 over mTORC2 signaling; increases lysosome acidification and increases cellular clearance of TDP-43 protein aggregates in a v-ATPase-dependent manner in U2OS osteosarcoma cells; inhibits mTORC1 signaling and enhances autophagy in mouse skeletal muscle and heart at 50 mg/kg

Formal name: N-[4-fluoro-3-[(1-oxo-2-propen-1-yl)amino]phenyl]-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide

Synonyms: 

Molecular weight: 368.3

CAS: 1808714-73-9

Purity: ≥95%

Formulation: A crystalline solid

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