EXH
EXH is a potent and versatile E3 ligase ligand utilized in the design and development of PROTACs (Proteolysis Targeting Chimeras). As a critical component in targeted protein degradation research, EXH binds selectively to the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex, enabling researchers to recruit VHL for the ubiquitination and subsequent degradation of disease-relevant target proteins. This VHL ligand is frequently employed in constructing bifunctional molecules for therapeutic and research applications, promoting innovative solutions in cancer, neurodegenerative, and other proteinopathy-centered studies. Ideal for medicinal chemistry and drug discovery projects, EXH provides researchers with a robust tool for advancing next-generation protein degradation technologies.
Structure of 2211116-16-2
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* For research and manufacturing use only. Not for human or clinical use.
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- Comprehensive PROTAC Platform
- Scientific Expertise & Technical Support
- Custom Synthesis & Design Service
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Background Introduction
EXH is a next-generation ligand designed specifically for E3 ubiquitin ligase engagement, playing a pivotal role in the development of advanced PROTACs (Proteolysis Targeting Chimeras). E3 ligase ligands, such as EXH, enable researchers and drug developers to harness the ubiquitin-proteasome system for targeted protein degradation. By facilitating the recruitment of a selected E3 ligase, EXH provides new opportunities for the chemical biology and pharmaceutical industries, especially in expanding the range of druggable proteins.
Mechanism
The mechanism of EXH centers on its high-affinity binding to a specific E3 ubiquitin ligase. Upon incorporation into a PROTAC molecule, EXH acts as the E3 ligase-recruiting moiety. It brings the fused E3 ligase into close proximity with a target protein, which is simultaneously bound by the PROTAC's target ligand. This proximity enables the transfer of ubiquitin molecules from the E2 enzyme to the target protein, flagging it for recognition and degradation by the 26S proteasome. The chemical design of EXH allows for efficient linker attachment, facilitating modular assembly into bifunctional degraders.
Applications
EXH is widely utilized in:
• PROTAC synthesis and optimization, especially in systems requiring E3 ligase engagement beyond conventional ligases like CRBN or VHL.• Structure-activity relationship (SAR) studies to explore E3 ligase selectivity and degradation efficiency in different cellular models.
• Drug discovery pipelines focusing on targeted protein degradation for undruggable or resistant protein targets.
• Development of tool compounds for elucidating ubiquitin-proteasome system biology and mechanisms of E3 ligase-mediated substrate recognition.
• Customizable conjugation strategies in both academic and commercial research projects aiming to expand the chemistry of protein degradation.
• 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
• High affinity for VHL E3 ligase enables efficient target protein ubiquitination and degradation.
• Optimized molecular structure facilitates seamless integration into custom PROTAC design workflows.
* 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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