EN6

Code: SML2689-25MG D2-231

Biochem/physiol Actions

EN6 is an autophagy activator that simultaneously upregulates lysosomal vacuolar H(+)-ATPase (v-ATPase) activity and induces its decoupling from the R...


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Biochem/physiol Actions

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.

assay≥98% (HPLC)
colorwhite to beige
formpowder
SMILES stringFC1=C(NC(C=C)=O)C=C(NC(C2=CN(C3=C(F)C=CC=C3)N=C2)=O)C=C1
solubilityDMSO: 2 mg/mL, clear
storage temp.2-8°C
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