3-Methyl-L-valyl-(4R)-4-hydroxy-N-{(1R)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl}-L-prolinamide

Background Introduction

3-Methyl-L-valyl-(4R)-4-hydroxy-N-{(1R)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl}-L-prolinamide is a highly potent VHL (von Hippel-Lindau) E3 ligase ligand that has been engineered for use in PROTAC (Proteolysis Targeting Chimera) research. VHL-based ligands are commonly used as building blocks in targeted protein degradation strategies, offering specificity, high binding affinity, and tunable linker sites that are crucial for optimizing PROTAC efficacy. This compound provides robust chemical handles for conjugating diverse payloads, making it a leading choice for advanced protein degradation research and drug development.

Mechanism

The compound functions by binding with high affinity to the VHL E3 ubiquitin ligase, a critical component in the ubiquitin-proteasome system. When linked to a target protein ligand via an appropriate linker, 3-Methyl-L-valyl-(4R)-4-hydroxy-N-{(1R)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl}-L-prolinamide recruits the VHL E3 ligase to the target protein. This proximity facilitates ubiquitination of the target, directing it to the proteasome for selective and efficient degradation. The unique structure of this ligand allows for modular synthesis, enabling precise control over linker length and orientation within PROTAC molecules.

Applications

This VHL E3 ligase ligand is a premier intermediate for constructing VHL-based PROTACs, empowering drug discovery and targeted protein degradation research. Key applications include:

• Synthesis of bifunctional PROTAC molecules targeting disease-relevant proteins
• Development of next-generation therapeutics for oncology, neurodegenerative, and inflammatory diseases
• Target validation, mechanistic studies, and structure-activity relationship (SAR) exploration in cellular assays
• Custom chemical biology tools for academic and pharmaceutical R&D projects

Researchers value this compound for its versatility, chemical stability, and compatibility with a wide array of target ligands, making it an essential reagent for the design and optimization of targeted protein degraders.

• 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
• Highly selective VHL E3 ligase ligand enhances the specificity and efficiency of targeted protein degradation in PROTAC applications.
• Well-defined chemical structure supports robust conjugation strategies, facilitating streamlined synthesis of next-generation PROTAC molecules.