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
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FOXA2 (HNF3B, TCF3B, Forkhead Box A2, OTTHUMP00000030409, MGC19807, OTTHUMP00000030410, Hepatic Nuclear Factor-3-beta, Hepatocyte Nuclear Factor 3, beta) (PE)