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About This Item
Empirical Formula (Hill Notation):
C19H14F2N4O2
CAS Number:
Molecular Weight:
368.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
FC1=C(NC(C=C)=O)C=C(NC(C2=CN(C3=C(F)C=CC=C3)N=C2)=O)C=C1
InChI key
SUSXQEYPNDORDQ-UHFFFAOYSA-N
Biochem/physiol Actions
Autophagy activator that upregulates lysosomal v-ATPase activity and induces its decoupling from Rag GTPases by covalently targeting v-ATPase subunit ATP6V1A Cys277.
EN6 is an autophagy activator that simultaneously upregulates lysosomal vacuolar H(+)-ATPase (v-ATPase) activity and induces its decoupling from the Rag GTPases by covalently targeting v-ATPase subunit ATP6V1A Cys277. EN6 blocks mTORC1 lysosomal recruitment & activation (1-4 hr 25 μM EN6 pretreatment prior to 10-min amino acids (AA) stimulation of AA-starived HEK293) and clears cellular TDP-43 aggregates (25 μM; U2OS with inducible TDP-43). When administered in mice in vivo (50 mg/kg ip.), EN6 inhibits mTORC1 signaling and activates autophagy in both skeletal muscle and heart tissue. Unlike bafilomycin A1 (BafA1), EN6 activates, but not inhibits v-ATPase catalytic activity.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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