(S,R,S)-AHPC-C4-NH2

Background Introduction

(S,R,S)-AHPC-C4-NH2 is a specialized E3 ligase ligand-linker conjugate widely used in the development of PROTACs (Proteolysis Targeting Chimeras). It incorporates the highly selective AHPC ligand, which is designed to recruit the von Hippel-Lindau (VHL) E3 ubiquitin ligase, and features a C4 polyethylene glycol (PEG4) linker, terminated with an aminated group for convenient conjugation.

Mechanism

The mechanism of (S,R,S)-AHPC-C4-NH2 centers on targeted protein degradation harnessed by the PROTAC system. The AHPC motif specifically binds to the VHL E3 ubiquitin ligase, while the C4-NH2 linker is engineered to be chemically connected to a ligand targeting the protein of interest. When assembled into a complete PROTAC molecule, (S,R,S)-AHPC-C4-NH2 brings the target protein into proximity with the E3 ligase, triggering ubiquitination and subsequent proteasomal degradation, thus enabling the selective elimination of disease-relevant proteins.

Applications

(S,R,S)-AHPC-C4-NH2 is extensively applied in the design and synthesis of PROTAC molecules for targeted protein degradation in drug discovery. It serves as a versatile intermediate for creating bifunctional compounds that degrade cancer-associated, inflammatory, or pathogenic proteins. Researchers utilize it for rapid profiling of protein function, the development of chemical biology tools, and the advancement of next-generation therapeutics. Its high binding affinity and modular linker design make it ideal for generating custom PROTACs relevant to oncology, neuroscience, and beyond.

• Amine-terminated linker enables efficient conjugation with target protein ligands for streamlined PROTAC assembly.
• Specifically designed for high-affinity VHL E3 ligase recruitment, enhancing targeted protein degradation applications.