(S,R,S)-AHPC-PEG₂-NH₂盐酸盐

Description

Protein degrader builiding block (S,R,S)-AHPC-PEG2-NH2(HCl salt) enables the synthesis of molecules fortargeted protein degradation andPROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation.When used with other protein degrader building blockswith a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.