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    1132709-15-9

    Catalog No. EBD4029810

    CAS 1132709-15-9

    Name [(1R)-3-methyl-1-({(2R)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid

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    Basic Information

    Synonyms: BortezomibDiastereomerRR

    Molecular Formula: C19H25BN4O4

    Molecular Weight: 384.24

    Categories: Medicinal Chemistry > Targeted Protein Degradation Tools > Target Protein Ligands Medicinal Chemistry > Targeted Protein Degradation Tools > Ligand-Linker Conjugates

    Product Description:
    This compound, known as ((R)-3-methyl-1-((R)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid, is a key chemical entity in the field of targeted protein degradation. It is a bortezomib derivative, specifically designed as a proteasome inhibitor and a ligand for the 20S proteasome. The structure features a boronic acid warhead, which is crucial for binding to the catalytic threonine residue of the proteasome's β5 subunit, and a peptide backbone that confers specificity. Its primary and most significant application is as a core component in the development of Proteolysis-Targeting Chimeras (PROTACs). In this role, it serves as the target protein ligand (or "warhead") that binds to the proteasome. When linked via a suitable linker to an E3 ubiquitin ligase recruiting moiety, it forms a complete PROTAC molecule. This bifunctional molecule can induce the ubiquitination and subsequent degradation of target proteins of interest, offering a novel therapeutic strategy beyond traditional inhibition. Due to its specific design for binding the proteasome and its integral function in constructing PROTAC degraders, it is classified as a specialized tool compound in chemical biology and drug discovery. It is not a general-purpose synthetic building block but a purpose-built ligand for a specific biological target within the degradation toolbox.
    Physical Properties
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