SML2689

EN6

≥98% (HPLC)

• Synonym(e): N-(3-Acrylamido-4-fluorophenyl)-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide, N-[4-Fluoro-3-[(1-oxo-2-propen-1-yl)amino]phenyl]-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide
• Empirische Formel (Hill-System): C₁₉H₁₄F₂N₄O₂
• CAS-Nummer: 1808714-73-9
• Molekulargewicht: 368.34
• MDL-Nummer: MFCD31665468
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 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

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable