Chemical structure of I-BET762 (GSK525762A).
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.
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.
Molecular Weight: 423.9 g/mol
Molecular Formula: C22H22ClN5O2
Solubility: Soluble in DMSO at 25 mg/ml or ethanol at 25 mg/ml.
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).
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