(S,R,S)-AHPC-amido-C5-acid is an advanced E3 Ligase Ligand-Linker Conjugate specifically engineered for PROTAC (Proteolysis Targeting Chimera) research and development. As a building block, it features the potent von Hippel-Lindau (VHL) E3 ligase-recruiting ligand, (S,R,S)-AHPC, covalently connected to a 5-carbon amido acid linker. This design enables efficient coupling to target protein ligands, allowing rapid assembly of customized PROTAC molecules.
Structure of 2162120-87-6
* For research and manufacturing use only. Not for human or clinical use.
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Background Introduction
(S,R,S)-AHPC-amido-C5-acid is a versatile E3 ligase ligand-linker conjugate commonly utilized in the construction of PROTACs (Proteolysis Targeting Chimeras). This compound features a well-characterized AHPC-based VHL ligand, an amide functionality, and a five-carbon linker terminated with a carboxylic acid group, enabling seamless conjugation to a variety of warheads targeting proteins of interest.
Mechanism
(S,R,S)-AHPC-amido-C5-acid operates by selectively recruiting the von Hippel-Lindau (VHL) E3 ubiquitin ligase complex through the AHPC ligand portion. The C5 linker offers optimal spatial orientation and flexibility, while the terminal carboxylic acid enables covalent attachment to protein-targeting ligands ('warheads'). When incorporated into a PROTAC molecule, this conjugate facilitates the formation of a ternary complex between the target protein and VHL E3 ligase, leading to ubiquitination and proteasomal degradation of the target protein.
Applications
(S,R,S)-AHPC-amido-C5-acid is widely used in the rational design and synthesis of VHL-based PROTACs for targeted protein degradation. Its modular structure makes it compatible with high-throughput screening and medicinal chemistry optimization to develop novel therapeutics across oncology, neurodegenerative diseases, and autoimmune disorders. This ligand-linker conjugate is an essential building block for researchers aiming to create potent and selective degraders for functional genomics studies, drug discovery, and translational research.
* 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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