An activator of autophagy
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EN6

Item No. 28715

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:10): 0.09 mg/mlDMSO: 15 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

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    25 mg

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    Product Description

    EN6 is an activator of autophagy.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chung, C.Y.-S., Shin, H.R., Berdan, C.A., et al. Covalent targeting of the vacuolar H+-ATPase activates autophagy via mTORC1 inhibition. Nat. Chem. Biol. 15, 776-785 (2019).