|Molecular Weight||366.4 g/mol|
|Solubility||Soluble in DMSO at 35 mg/mL.|
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 IC50 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).
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