VH 032 amide-alkylC9-acid

Background Introduction

VH 032 amide-alkylC9-acid is a specialized E3 ligase ligand-linker conjugate, meticulously designed to facilitate the construction of PROTACs (Proteolysis Targeting Chimeras). This molecule incorporates the VH 032 moiety, which specifically binds to the von Hippel-Lindau (VHL) E3 ubiquitin ligase, combined with an amide-alkylC9-acid linker, offering optimal flexibility and spacing for efficient target protein degradation. As the demand for targeted protein degradation technology rises in medicinal chemistry and drug discovery, VH 032 amide-alkylC9-acid proves to be an essential building block.

Mechanism

VH 032 amide-alkylC9-acid operates as a bifunctional molecule, where the VH 032 portion binds selectively to the VHL E3 ligase. The amide-alkylC9-acid linker provides customizable length and chemical versatility, enabling convenient conjugation to a variety of target protein ligands. When incorporated into a PROTAC, this conjugate serves to recruit the E3 ligase to the protein of interest, triggering its ubiquitination and subsequent proteasomal degradation. This precise mechanism facilitates the targeted removal of disease-associated proteins within cells.

Applications

VH 032 amide-alkylC9-acid is widely used in the synthesis of VHL-based PROTACs for research and pharmaceutical development. Its customizable linker supports optimization of PROTAC designs targeting diverse proteins implicated in cancer, neurodegeneration, and other diseases. This conjugate enables researchers to develop next-generation therapeutics by harnessing the cell's natural proteolysis machinery, opening new avenues in drug discovery, chemical biology, and functional proteomics.

• Long alkyl C9 linker provides optimal spatial orientation for effective VHL recruitment in PROTAC design.
• Amide-terminated structure offers robust functionalization options, enabling versatile conjugation for targeted protein degradation.