PT-179

Background Introduction

PT-179 is a highly selective and cell-permeable ligand designed to recruit the von Hippel-Lindau (VHL) E3 ubiquitin ligase. As a key component in the development of PROTACs (Proteolysis Targeting Chimeras), PT-179 serves as a strategic VHL ligand, enabling targeted protein degradation (TPD) strategies for research and drug discovery. By incorporating optimally placed functional groups, PT-179 offers enhanced binding affinity, chemical stability, and synthetic utility for generating innovative bifunctional degraders.

Mechanism

PT-179 acts as a potent VHL E3 ligase ligand, binding to the VHL protein within the CUL2-VHL E3 ubiquitin ligase complex. Once conjugated to a suitable ligand for a protein of interest, PT-179 facilitates the formation of a ternary complex, bringing together the VHL E3 ligase and the target protein. This proximity triggers ubiquitination of the target protein, marking it for recognition and degradation by the 26S proteasome. PT-179's chemical structure allows flexible linker attachment, making it ideal for constructing PROTAC molecules with robust efficacy and specificity.

Applications

PT-179 is widely utilized in the synthesis and development of VHL-based PROTACs and heterobifunctional degraders. Its application areas include:

• Generation of bifunctional molecules for selective protein degradation in cellular and in vivo models.
• Custom synthesis of VHL E3 ligase ligands for PROTAC library construction and SAR studies.
• Drug discovery programs focused on 'undruggable' targets through targeted protein degradation.
• Tool compound for mechanistic studies exploring VHL-mediated E3 ligase activity.
• Academic and pharmaceutical research for validating novel disease targets and advancing therapeutic lead identification.

PT-179's versatility and reliability position it as a preferred choice for researchers seeking to develop next-generation degradation-based therapeutics.

• 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 enables precise protein degradation in targeted PROTAC applications.
• Optimized for enhanced cell permeability and stability, facilitating efficient PROTAC design and development.