VH032-C6-NH-Boc

Background Introduction

VH032-C6-NH-Boc is a derivative of the VHL (von Hippel-Lindau) E3 ubiquitin ligase ligand, equipped with a hexamethylene (C6) linker terminated with a Boc-protected amine. VH032 is a well-established small-molecule ligand that binds selectively to the VHL E3 ligase, a crucial component in PROTAC-based targeted protein degradation. The C6 linker and Boc-protected amine facilitate synthetic flexibility, making this compound an excellent starting point for constructing VHL-based PROTACs and related chemical biology tools.

Mechanism

VH032-C6-NH-Boc functions by specifically binding to the VHL E3 ubiquitin ligase within the CUL2-VHL E3 ligase complex. When connected to a ligand for a protein of interest, this molecule forms the basis of a bifunctional PROTAC, enabling the recruitment of VHL to the target protein. This proximity leads to the ubiquitination and subsequent proteasomal degradation of the target. The hexamethylene (C6) linker offers optimal spatial separation, while the Boc-protected amine allows further functionalization or selective deprotection during PROTAC assembly.

Applications

VH032-C6-NH-Boc is primarily used as a key intermediate for synthesizing VHL-recruiting PROTACs, supporting targeted protein degradation research. Its applications include:

• Development of VHL ligase-recruiting PROTACs for therapeutic discovery
• Structure-activity relationship (SAR) studies for PROTAC optimization
• Synthesis of chemical probes for target validation in cell-based assays
• Medicinal chemistry research for developing next-generation protein degraders
• Customizable linker design for tailored degrader synthesis in CRO and academic settings

Overall, VH032-C6-NH-Boc is an essential reagent for driving innovation in PROTAC technology and targeted protein degradation.

• 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
• Optimized for efficient VHL E3 ligase recruitment, enhancing targeted protein degradation in PROTAC applications.
• Boc-protected amine design increases synthetic flexibility and enables easy customization for novel PROTAC development.