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EN6

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].

Product Specifications

CAS Number

[1808714-73-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy

Type

Reference compound

Related Pathways

Autophagy

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/en6.html

Purity

99.42

Solubility

DMSO : 5 mg/mL (ultrasonic) |Ethanol : 1.11 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=CN(C2=CC=CC=C2F)N=C1)NC3=CC=C(F)C(NC(C=C)=O)=C3

Molecular Formula

C19H14F2N4O2

Molecular Weight

368.34

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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