(S,R,S)-AHPC-C1-Br

Background Introduction

(S,R,S)-AHPC-C1-Br is a specialized E3 ligase ligand-linker conjugate widely utilized in the development of PROTAC (Proteolysis Targeting Chimera) molecules. This compound is designed to bind the von Hippel-Lindau (VHL) E3 ligase, which plays a pivotal role in targeted protein degradation technologies for both research and drug discovery.

Mechanism

(S,R,S)-AHPC-C1-Br functions as a modular component in PROTAC design by harnessing its high affinity for the VHL E3 ligase. The AHPC moiety acts as a VHL ligand, while the C1-branched linker provides an adaptable attachment point for heterobifunctional conjugation. When incorporated into a PROTAC, this conjugate bridges the E3 ligase and a target protein via a custom-designed warhead. This proximity induces ubiquitination of the target protein, ultimately leading to its recognition and degradation by the proteasome.

Applications

(S,R,S)-AHPC-C1-Br is instrumental in the rational design and synthesis of VHL-based PROTACs for the study and therapeutic targeting of disease-relevant proteins. Its applications include the creation of protein degraders for cancer research, validation of disease targets, and the development of next-generation targeted therapies. This conjugate is also valuable in constructing custom PROTAC libraries and advancing small molecule-induced protein degradation strategies in both academic and pharmaceutical industry settings.