VH032-CH2-Boc

Background Introduction

VH032-CH2-Boc is a derivative of the well-established von Hippel-Lindau (VHL) E3 ligase ligand, VH032. The introduction of a tert-butoxycarbonyl (Boc) protected aminomethyl group at the VH032 structure provides a versatile conjugation site with improved stability for solid-phase and solution-phase synthesis, making this compound highly valuable in the design and optimization of proteolysis targeting chimeras (PROTACs) for targeted protein degradation research.

Mechanism

VH032-CH2-Boc functions as a selective VHL E3 ligase ligand, engaging the VHL component of the CUL2 E3 ubiquitin ligase complex. Upon binding, this ligand recruits VHL to the desired target protein when linked via a bifunctional PROTAC molecule. This proximity enables the transfer of ubiquitin molecules to the target protein, marking it for recognition and degradation by the 26S proteasome. The Boc-protected aminomethyl group serves as a chemical handle for introducing diverse linkers and facilitates downstream deprotection and conjugation strategies in PROTAC synthesis.

Applications

VH032-CH2-Boc is widely utilized in the development of VHL-based PROTACs for preclinical and translational protein degradation studies. Key applications include:

• Construction of bifunctional molecules for targeted protein degradation via VHL recruitment
• Medicinal chemistry optimization and structure-activity relationship (SAR) exploration
• Synthesis of focused PROTAC libraries targeting key disease-related proteins
• Custom chimeric molecule assembly for pharmaceutical and academic drug discovery projects

With its protected functional group, VH032-CH2-Boc allows for robust linker attachment and flexible integration into various chemical scaffolds, supporting efficient and scalable synthetic workflows in the field of 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
• Boc-protected amine group provides enhanced chemical stability and controlled deprotection for efficient synthetic workflows.
• Optimized for VHL-based PROTAC development, enabling selective targeting and degradation of disease-relevant proteins.