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Commit: 3c1f305a63297e594ac8d7bb5424007d592d68be
XML generation date: 2024-09-20 06:23:30.451
Product last modified at: 2024-07-10T22:00:09.196Z
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PDP - Template Name: Chemical Modulators
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  1. Products /
  2. Activators & Inhibitors /
  3. SB-525334

SB-525334 #20090

    Product Information

    Product Usage Information

    SB-525334 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.97 mL 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 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 343.4 g/mol
    Purity >99%
    Molecular Formula C21H21N5
    CAS 356559-20-1
    Solubility Soluble in DMSO at 30 mg/mL.

    Background

    The small-molecule SB-525334 inhibits transforming growth factor-β1 receptor (TGF-βR1, ALK5) with an IC50 of 14.3 nM. SB-525334 also inhibits the related receptor ALK4 (IC50 = 58.5 nM) but is inactive against ALK2, ALK3, and ALK6. Inhibition of TGF-β downstream signaling by SB-525334 blocks phosphorylation and nuclear translocation of Smad2/3 protein and reduces PAI-1 and procollagen α1(I) mRNA expression in renal epithelial carcinoma cells (1). SB-525334 treatment of a bleomycin-induced pulmonary fibrosis model reduced TGF-β-mediated nuclear translocation of Smad2/3, decreased myofibroblast proliferation, and attenuated pulmonary fibrosis (2). Exposure of mesenchymal and epithelial tumors in Eker rats to SB-525334 reduced the size and number of mesenchymal tumors but had the opposite effect on epithelial cancer cells and lesions (3). Inhibition of ALK5 by SB-525334 in both human pulmonary artery smooth muscle cells and a rat model of pulmonary arterial hypertension resulted in decreased sensitivity to TGF-β, and attenuated pulmonary arterial pressure and right ventricular hypertrophy (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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