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Autophagy activator EN6

Chemical Structure : Autophagy activator EN6

CAS No.: 1808714-73-9

Autophagy activator EN6 (EN6)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 368.344
Formula C19H14F2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-acrylamido-4-fluorophenyl)-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide

References

1. Chung CY, et al. Nat Chem Biol. 2019 Jul 8. doi: 10.1038/s41589-019-0308-4.

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