(S,R,S)-AHPC-Me

Description: (S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM. Target: Ligand for E3 Ligase. Smiles: C([C@H](C(C)(C)C)N)(=O)N1[C@H](C(N[C@@H](C)C2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@@H](O)C1. References: Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28,113(26):7124-9.