VH032-C3-Boc

Background Introduction

VH032-C3-Boc is a derivative of the VH032 ligand, a validated small molecule that specifically binds to the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. The C3-Boc modification incorporates a three-carbon linker terminated with a tert-butoxycarbonyl (Boc) protecting group, enhancing chemical stability and facilitating further linker derivatization. VH032-based ligands are crucial building blocks in the design and synthesis of PROTACs (Proteolysis Targeting Chimeras) due to their high affinity and specificity for the VHL E3 ligase.

Mechanism

VH032-C3-Boc recruits the VHL E3 ubiquitin ligase by binding to the VHL protein, a substrate recognition component of the CUL2-VHL E3 ligase complex. When integrated into a PROTAC, this ligand joins a target protein ligand via a bifunctional linker, resulting in the formation of a ternary complex between the target protein, the PROTAC, and VHL. This complex brings the target protein into proximity with the E3 ligase, facilitating its ubiquitination and subsequent proteasomal degradation. The Boc-protected C3 linker enables modular synthetic strategies for the incorporation of various functional groups essential for PROTAC optimization.

Applications

VH032-C3-Boc serves as a highly effective intermediate for generating VHL-recruiting PROTACs and molecular glue degraders. Key applications include:

• Synthesis of VHL-based PROTACs for targeted protein degradation studies
• Design of custom linker strategies in medicinal chemistry projects
• Structure-activity relationship (SAR) analysis in degrader development pipelines
• Assembly of bifunctional molecules for drug discovery, target validation, and preclinical research

This compound is especially valuable for scientists engaged in PROTAC platform advancement, enabling the precise construction of E3 ligase recruiter modules for a wide spectrum of therapeutic targets.

• High-purity compound verified by HPLC, NMR, and LC-MS
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• Boc-protected linker improves solubility and synthetic versatility for PROTAC assembly.
• Highly selective for VHL E3 ligase, enabling efficient and targeted protein degradation applications.