Product Description
Chemical Modulators for studying in the research area.
Product Usage Information
BRD-7389 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.91 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 .
Background
The inhibitor BRD-7389 was originally isolated by screening a set of small molecules for detection of insulin protein production in a murine pancreatic α-cell line. BRD-7389 treatment of cells resulted in a dose-dependent increase in Ins2 mRNA and a number of β-cell markers. Similar results were seen in primary human islet cells. Further studies determined that BRD-7389 inhibited a number of protein kinases, and was most active against 90 kDa ribosomal S6 kinase (RSK) family members, with IC values of 1.5 mM, 2.4 mM, and 1.2 mM for RSK1, RSK2, and RSK3, respectively (1). BRD-7389 inhibited RSK activity and blocked cell proliferation in colon cancer cells stimulated by muscarinic acetylcholine receptor activation (2). BRD-7389 and the unrelated RSK inhibitor BI-D1870 inhibited protein synthesis and cell proliferation in multiple dual-resistant melanoma patient-derived cells, suggesting a possible strategy in the treatment of drug-resistant melanoma (3).
Alternate Names
1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione
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Collaboration
Tony Tang
Email: Tony.Tang@iright.com
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