NBE5 is an orally active hydrophobic tag-targeting degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C)[1].
Molekulargewicht:
780.13
Formel:
C50H73N3O4
Target-Kategorie:
HSP,Keap1-Nrf2,PROTACs
Anwendungsbeschreibung:
MCE Product type: Reference compound
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