VH032-C2-NH-Boc

Background Introduction

VH032-C2-NH-Boc is a chemically engineered ligand designed to interact specifically with the von Hippel-Lindau (VHL) E3 ubiquitin ligase. VHL ligands have emerged as essential building blocks in the field of targeted protein degradation, particularly in the assembly of PROTACs (Proteolysis Targeting Chimeras). The VH032 scaffold is renowned for its high affinity and selectivity for the VHL component within the E3 ligase complex, while the C2 linker and Boc-protected amine offer robust conjugation chemistry and synthetic flexibility during PROTAC development.

Mechanism

VH032-C2-NH-Boc functions by binding to the VHL E3 ubiquitin ligase, recruiting the ligase complex to the target protein when incorporated into bifunctional molecules like PROTACs. The ligand's core structure enables precise docking onto VHL, while the C2 linker facilitates optimal spatial orientation between the E3 ligase and the target protein ligand. The Boc-protected amine ensures stability during synthetic steps and can be easily deprotected to enable downstream coupling reactions. This modularity supports efficient and effective assembly of customized PROTACs for protein degradation.

Applications

VH032-C2-NH-Boc is widely utilized in medicinal chemistry and chemical biology for constructing VHL-recruiting PROTACs, enabling controlled and selective degradation of target proteins via the ubiquitin-proteasome system. Key applications include:

• Synthesis of next-generation PROTAC molecules for drug discovery and mechanistic studies
• Development of tool compounds for target validation and functional genomics
• Constructing covalent or reversible VHL-based molecular glues
• Optimization of PROTAC linker length and composition during structure-activity relationship (SAR) research
• Facilitating custom PROTAC or molecular glue synthesis for pharmaceutical and academic research projects

• 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 amine enhances synthetic flexibility for diverse PROTAC designs.
• Optimized for efficient VHL E3 ligase recruitment in targeted protein degradation studies.