VH032-O-C2-NH-Boc is an optimized ligand for VHL (Von Hippel-Lindau) E3 ligase, designed for use in PROTAC (Proteolysis Targeting Chimera) research and development. As an "E3 Ligase Ligand," it features a Boc-protected amine and an extended ethylene glycol linker, facilitating conjugation to various target protein ligands. VH032-based ligands are central in designing VHL-recruiting PROTACs, enabling selective ubiquitination and degradation of disease-causing proteins. This compound is ideal for scientists developing next-generation protein degraders targeting oncology, neurodegenerative disorders, and other therapeutic areas.
Structure of 2409007-41-4
* For research and manufacturing use only. Not for human or clinical use.
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Background Introduction
VH032-O-C2-NH-Boc is a derivative of the well-established VHL (Von Hippel-Lindau) E3 ubiquitin ligase ligand VH032, functionalized with a Boc (tert-butoxycarbonyl)-protected amine at the end of a flexible ethylene linker. The VHL-recruiting chemotype is a cornerstone in PROTAC (Proteolysis Targeting Chimera) and targeted protein degradation research, thanks to its high affinity and selectivity for the VHL E3 ligase complex. This modification enables efficient PROTAC design by offering a convenient functional handle for linker diversification and conjugation strategies.
Mechanism
VH032-O-C2-NH-Boc specifically binds to the VHL E3 ubiquitin ligase, hijacking the natural ubiquitination machinery to direct target proteins for proteasomal degradation. The ethylene linker and terminal Boc-protected amine provide flexible options for conjugation to various ligands targeting proteins of interest. The Boc group not only protects the reactive amine functionality during synthetic processes but also increases the compound's stability and synthetic versatility, streamlining the generation of heterobifunctional degraders.
Applications
VH032-O-C2-NH-Boc is an ideal intermediate for the synthesis of VHL-based PROTACs and related degraders. Key application areas include:
• Construction of VHL-recruiting E3 ligase ligands for PROTACs targeting diverse proteins
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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