VH-298

Background Introduction

VH-298 is a potent, cell-permeable small molecule ligand selectively targeting the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. As a widely used VHL ligand, VH-298 forms a key component in the design and synthesis of VHL-based PROTACs (Proteolysis Targeting Chimeras), supporting advanced strategies in targeted protein degradation (TPD) for drug discovery, chemical biology, and therapeutic development.

Mechanism

VH-298 binds with high affinity to the VHL substrate recognition site within the CUL2-VHL E3 ligase complex. This binding event facilitates the recruitment of VHL to the PROTAC heterobifunctional molecule, allowing for the selective ubiquitination and subsequent proteasomal degradation of the intended target protein. The precise and stable interaction profile of VH-298 with VHL ensures robust E3 ligase engagement, providing efficient degradation of proteins deemed as 'undruggable' by traditional approaches.

Applications

VH-298 is regarded as a gold-standard VHL ligand in the construction of next-generation PROTACs and degraders. Its utility includes:

• Synthesis of VHL-recruiting PROTACs for targeted protein knockdown
• Design and optimization of bifunctional degraders in target validation screening
• PROTAC SAR (Structure-Activity Relationship) studies for fine-tuning degradation efficiency
• Application in chemical biology to elucidate novel protein degradation pathways
• Custom PROTAC library creation for pharmaceutical and academic research

VH-298's reliable E3 ligase recruitment properties make it indispensable for accelerating research in targeted protein degradation, drug discovery, and precision medicine.

• 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
• High affinity and selectivity for VHL E3 ligase, ensuring efficient target protein degradation in PROTAC applications.
• Well-characterized ligand with robust data supporting its use in VHL-based PROTAC design, enabling accelerated drug discovery projects.

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	1.91 mL	9.55 mL	19.1 mL
5 mM	0.38 mL	1.91 mL	3.82 mL
10 mM	0.19 mL	0.95 mL	1.91 mL
50 mM	0.04 mL	0.19 mL	0.38 mL