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  3. MZ1

MZ1 #34751

    Product Information

    Product Usage Information

    MZ1 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute 5 mg of powder in 997 μL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

    Storage

    Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 2 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 1002.6 g/mol
    Purity >98%
    Molecular Formula C49H60ClN9O8S2
    CAS 1797406-69-9
    Solubility Soluble in DMSO at 100 mg/mL.

    Background

    The MZ1 compound is a proteolysis-targeting chimera (PROTAC) degrader of bromodomain-containing protein 4 (BRD4) (1). MZ1 is composed of a bromodomain inhibitor (JQ1) bound to a ligand that recruits the von Hippel-Lindau (VHL) E3 ubiquitin ligase (1). This ligase is part of a complex that works to regulate the cellular response to oxygen levels and target specific proteins for degradation (2). By binding to this ligase and then to BRD4 bromodomains, MZ1 tags the protein for degradation (1). The BRD4 protein is an epigenetic regulator involved in gene expression and transcription regulation, often found to be overactive in several cancers, including breast and leukemias (3). The ability of BRD4 to attach to acetylated histones at promoters and enhancers is a focus in clinical research, as these actions can drive uncontrolled cancer growth (3). MZ1 has also been shown to exert anticancer effects in acute myeloid leukemia (AML), as BRD4 degradation leads to c-Myc downregulation, which is critical for AML survival (4). The median IC50 for BRD4 is 49 nM. It is effective at lower concentrations ranging from 5 to 150 nM (5).

    Limited Uses

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    Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

    For Research Use Only. Not for Use in Diagnostic Procedures.
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