VH032-PEG2-NH-Boc

Background Introduction

VH032-PEG2-NH-Boc is a derivative of VH032, a well-established ligand for the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex, which is commonly used in proteolysis-targeting chimera (PROTAC) development. This compound features a polyethylene glycol (PEG2) spacer and a Boc-protected amino group, facilitating versatile conjugation for linker attachment and PROTAC construction. Its unique structure enables enhanced solubility, flexibility, and functionalization, making it highly attractive for researchers designing VHL E3 ligase-based degraders.

Mechanism

VH032-PEG2-NH-Boc binds with high affinity to the VHL E3 ligase, an essential component of the cellular ubiquitin-proteasome system responsible for tagging proteins for degradation. The PEG2 spacer confers increased molecular flexibility and aqueous solubility, while the terminal Boc-protected amine serves as a functional handle for deprotection and subsequent conjugation. When used as part of a PROTAC molecule, VH032-PEG2-NH-Boc tethers VHL to a designated target protein ligand. This proximity induces the ubiquitination and selective proteasomal degradation of the target protein within cells.

Applications

VH032-PEG2-NH-Boc is extensively utilized in the discovery and development of VHL-based PROTACs and bifunctional protein degraders. The product supports:

• PROTAC synthesis: Acts as the VHL E3 ligase ligand in the assembly of degraders targeting a variety of disease-associated proteins.
• Structure-activity relationship (SAR) exploration: Enables linker optimization through flexible PEG2 spacing and ease of amine deprotection/conjugation.
• Target validation: Facilitates research in targeted protein degradation for drug discovery projects and mechanism-of-action studies.
• Medicinal chemistry and chemical biology: Serves as a key intermediate for generating novel VHL-recruiting molecules in both academic and CRO settings.

• 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
• Flexible PEG2 linker enhances solubility and bioavailability for efficient PROTAC design.
• Boc-protected amine allows for selective and straightforward conjugation to target ligands or payloads.