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    1268524-71-5

    Catalog No. EBD3059212

    CAS 1268524-71-5

    Name ()-JQ1

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    Basic Information

    Synonyms: (-)-JQ-1 (-)-JQ1 ()-JQ1 (R)-(-)-tert-Butyl2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate

    Molecular Formula: C23H25ClN4O2S

    Molecular Weight: 456.99

    Categories: Medicinal Chemistry > APIs and Their Salts > Antineoplastic Agents Medicinal Chemistry > Targeted Protein Degradation Tools > Target Protein Ligands

    Product Description:
    (R)-JQ1 is a potent, cell-permeable, and selective small-molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, specifically targeting the first bromodomain (BD1) of BRD4. It functions by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains, thereby displacing them from chromatin and suppressing the transcription of key oncogenes such as *MYC*. This compound is a widely used chemical probe and a lead compound in oncology research for studying the role of BET proteins in cancer, inflammation, and other diseases. It has demonstrated significant anti-proliferative activity in various cancer cell lines and animal models, particularly in hematological malignancies like acute myeloid leukemia (AML) and multiple myeloma. Beyond its role as a direct inhibitor, (R)-JQ1 serves as a foundational ligand for the development of proteolysis-targeting chimeras (PROTACs) aimed at degrading BET proteins. Due to its high specificity and well-characterized mechanism, (R)-JQ1 is a staple tool in epigenetic and transcriptional regulation research. It is typically handled as a research-grade chemical and is not approved for therapeutic use in humans.
    Physical Properties
    mg g kg ml l t