VH032-NH-CO-CH2-NHBoc

Background Introduction

VH032-NH-CO-CH2-NHBoc is a derivative of the well-established VH032, a synthetic ligand for the von Hippel-Lindau (VHL) E3 ubiquitin ligase. VHL-based E3 ligase ligands are among the most commonly utilized warheads in PROTAC (Proteolysis Targeting Chimera) design, enabling targeted protein degradation for research and drug discovery. The unique NH-CO-CH2-NHBoc modification on VH032 offers a protected amino group for linker attachment, enhancing flexibility and efficiency in synthesizing bifunctional molecules.

Mechanism

VH032-NH-CO-CH2-NHBoc works by selectively binding to the VHL E3 ubiquitin ligase complex through its VH032 scaffold. When incorporated into PROTACs, this ligand recruits VHL to form a ternary complex with the target protein ligand, enabling ubiquitination of the target protein and subsequent degradation by the proteasome. The NHBoc-protected amine on the linker region allows orthogonal deprotection strategies, facilitating precise chemical conjugation during PROTAC assembly and offering streamlined synthesis routes.

Applications

VH032-NH-CO-CH2-NHBoc is widely used as a chemical tool and intermediate in the development of VHL-recruiting PROTACs and targeted protein degraders. Its optimized linker with Boc-protected amine enables straightforward coupling to a broad range of target ligands for the construction of potent and selective bifunctional degraders. Key applications include:

• Design and synthesis of VHL-based PROTACs for drug discovery and target validation
• Structure-activity relationship (SAR) studies and medicinal chemistry optimization of degraders
• Customizable platform for linking diverse protein-targeting moieties in academic and pharmaceutical research
• CRO/CMO synthesis of next-generation targeted protein degraders and related chemical biology probes

• 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 stability and facilitates downstream functionalization in PROTAC synthesis.
• Optimized for targeting VHL E3 ligase, enabling efficient protein degradation in targeted therapeutic research.