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Render Timestamp: 2024-12-19T20:42:03.294Z
Commit: f2d32940205a64f990b886d724ccee2c9935daff
XML generation date: 2024-04-24 09:10:49.000
Product last modified at: 2024-12-17T18:55:09.798Z
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PDP - Template Name: Chemical Modulators
PDP - Template ID: *******c501c72
  1. Products /
  2. Activators & Inhibitors /
  3. I-BET762 (GSK525762A)

I-BET762 (GSK525762A) #45122

    Product Information

    Product Usage Information

    I-BET762 (GSK525762A) is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.17 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 423.9 g/mol
    Purity >98%
    Molecular Formula C22H22ClN5O2
    CAS 1260907-17-2
    Solubility Soluble in DMSO at 25 mg/ml or ethanol at 25 mg/ml.

    Background

    I-BET762 (GSK525762A) is a potent BET bromodomain inhibitor, as well as a downregulator of the critical oncogene, MYC (1,5). This small molecule inhibits binding of acetylated histones to BET proteins, disrupting the expression of inflammatory genes in activated macrophages, as well as blocking acute inflammation in mice (2,3). Studies have found that I-BET762 (GSK525762A) suppressed T cell inflammation resulting in upregulated expression of anti-inflammatory gene products, and downregulated expression of several proinflammatory cytokines (3). I-BET762 (GSK525762A) has also been shown to induce cell death and suppress cell proliferation in pancreatic ductal adenocarcinoma (PDAC) cells (4).

    限制使用

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