ALV2 is a synthetic ligand optimized for binding to the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex. As an advanced E3 Ligase Ligand, ALV2 is widely used in PROTAC (Proteolysis Targeting Chimera) research for targeted protein degradation. By incorporating ALV2 into bifunctional molecules, researchers can recruit the VHL E3 ligase to specific target proteins, enabling their ubiquitination and subsequent proteasomal degradation. This mechanism empowers the development of next-generation therapeutics for previously 'undruggable' targets, supporting innovative cancer, neurodegeneration, and inflammation studies. ALV2 offers high binding affinity and synthetic flexibility, making it an essential tool for medicinal chemistry, chemical biology, and drug discovery efforts focused on targeted protein degradation pathways.
Structure of 2438124-95-7
* For research and manufacturing use only. Not for human or clinical use.
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Background Introduction
ALV2 is a potent and selective small molecule ligand designed to bind the Von Hippel-Lindau (VHL) E3 ubiquitin ligase. VHL ligands are essential components in the PROTAC (Proteolysis Targeting Chimera) technology landscape, facilitating targeted protein degradation by leveraging the endogenous ubiquitin-proteasome system. ALV2 features an optimized structure that offers improved binding affinity and synthetic adaptability, making it a preferred choice for constructing next-generation VHL-based PROTACs.
Mechanism
ALV2 works by specifically engaging the VHL E3 ligase, enabling the recruitment of the CUL2-VHL E3 ubiquitin ligase complex. When appended to a target protein ligand via a suitable linker, ALV2 forms the E3 ligase recruitment module of a PROTAC molecule. This bifunctional chimera brings the target protein into close proximity with the VHL ligase complex, triggering polyubiquitination and subsequent proteasomal degradation of the protein of interest. The rationally engineered features of ALV2 provide expanded linker design and attachment options, supporting efficient PROTAC construction and enhanced degradation activity.
Applications
ALV2 is widely used in the development of VHL-recruiting PROTACs for preclinical and clinical research applications such as:
• Synthesis of bispecific protein degraders targeting disease-relevant proteins (kinases, transcription factors, etc.)
* 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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