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XML generation date: 2024-09-20 06:23:31.641
Product last modified at: 2024-08-30T22:45:08.134Z
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PDP - Template Name: Chemical Modulators
PDP - Template ID: *******c501c72
  1. Products /
  2. Activators & Inhibitors /
  3. PRT-4165

PRT-4165 #92443

    Product Information

    Product Usage Information

    PRT-4165 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 1 mg of powder in 0.43 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

    Storage

    Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 235.2 g/mol
    Purity >98%
    Molecular Formula C15H9NO2
    CAS 31083-55-3
    Solubility Soluble in DMSO at 25 mg/mL or ethanol at 6 mg/mL.

    Background

    The small-molecule PRT-4165 inhibits the E3 ligase activity of Bmi1/Ring1A (IC50 = 3.9 μM), inhibits ubiquitination of topoisomerase Top2α, and alters Bmi1 localization from nucleolar bodies to more disperse nuclear and cytoplasmic localizations (1). PRT-4165 inhibits both Ring1A and RNF2 (Ring1B), which account for the polycomb-repressive complex 1 (PRC1) E3 ubiquitin ligase activity. PRC1-mediated ubiquitylation of histones plays an important role in DNA repair and gene silencing, and may be relevant in determining cell fate and development of human cancers. Treatment of cells with PRT-4165 inhibited H2A ubiquitylation in cells and at sites of DNA damage, resulting in delayed double-strand break (DSB) repair and impaired response to genotoxic stress (2). PRT-4165 treatment of leukemia cells suppressed cell growth and downregulated NOTCH signaling protein expression (3). PRT-4165 treatment of differentiating human embryonic stem cells promoted neuroectodermal differentiation, indicating that Ring1B regulation could be used to direct stem cells toward an early neuronal fate (4).

    Limited Uses

    Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

    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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