(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.
(S,R,S)-AHPC-amido-C5-acid is a versatile E3 Ligase Ligand-Linker Conjugate used in the development of PROTACs, facilitating targeted protein degradation by linking an E3 ligase to a target protein. The following provides a detailed description of this molecule, including its linker, ligand, and recommended target protein ligand.
Linker: The linker in this molecule is a C5 aliphatic chain, providing moderate length and flexibility, which ensures optimal spatial arrangement between the ligand and the target protein. It is non-cleavable, offering stability during the degradation process.
Ligand: The ligand is derived from AHPC, a potent and selective E3 ligase binder. Its stereochemistry, specifically the (S,R,S) configuration, enhances binding affinity and specificity, making it highly effective for targeted protein degradation applications.
Reactive Site: The reactive site of this molecule is an amido group, which facilitates coupling with the target protein ligand through amide bond formation. This site is suitable for reactions such as peptide coupling, ensuring stable and efficient conjugation.
Recommended Target Protein Ligand: The recommended warhead for this molecule is a small-molecule inhibitor with a reactive functional group capable of forming a stable covalent bond with the amido group. This compatibility ensures precise targeting and degradation of disease-related proteins, making it ideal for experimental studies in drug discovery and development.
* 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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