(S,R,S)-AHPC-Me dihydrochloride targets the von Hippel-Lindau (VHL) protein as a ligand for E3 ligase recruitment. This compound serves as a critical precursor for the synthesis of ARV-771, a PROTAC degrader that utilizes the VHL E3 ligase to facilitate the degradation of BET proteins. It has demonstrated potent activity in degrading BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM, highlighting its potential for therapeutic applications in cancer research.
(S,R,S)-AHPC-Me dihydrochloride targets the von Hippel-Lindau (VHL) protein as a ligand for E3 ligase recruitment. This compound serves as a critical precursor for the synthesis of ARV-771, a PROTAC degrader that utilizes the VHL E3 ligase to facilitate the degradation of BET proteins. It has demonstrated potent activity in degrading BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM, highlighting its potential for therapeutic applications in cancer research.
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