Name | bas 05532738 |
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Synonyms | hms1493i11 |
Description | BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells[1]. |
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Related Catalog | |
Target |
RSK1:1.5 μM (IC50) RSK2:2.4 μM (IC50) RSK3:1.2 μM (IC50) CDK5/p35:6.5 μM (IC50) DRAK1:2.8 μM (IC50) FLT3:3.5 μM (IC50) PIM1:3.7 μM (IC50) PKG1α:6.5 μM (IC50) SGK:13.8 μM (IC50) |
In Vitro | BRD7389 (0.425-6.8 μM) induces insulin expression in mouse α-cells after 3 days treatment. BRD7389 induces a dose-dependent up-regulation of insulin (Ins2) mRNA, peaking at 0.85 μM; 5 days treatment with BRD7389 results in greater induction of insulin gene expression, about 50-fold at 0.85 μM[1]. BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line[1]. BRD7389 also increases β-cell-specific gene expression in primary human islet cells[1]. BRD7389 (1 μM; added 30 min prior to Carbachol treatment 48 h) fully abolishes carbachols timulated cell proliferation, but has little effect on the basal level of proliferation[2]. RT-PCR[1] Cell Line: Mouse α-cell line Concentration: 0.425, 0.85, 1.7, 3.4, 6.8 μM Incubation Time: 3 days and 5 days Result: Up-regulated expression of Pdx1. Cell Proliferation Assay[2] Cell Line: SNU-407 colon cancer cell Concentration: 1 μM Incubation Time: Added 30 min prior to Carbachol treatment (48 h) Result: Almost completely blocked Carbachol (1 mM)-stimulated cell proliferation. |
References |
Molecular Formula | C24H18N2O2 |
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Molecular Weight | 366.41200 |
Exact Mass | 366.13700 |
PSA | 62.22000 |
LogP | 4.87940 |
Hazard Statements | H413 |
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RIDADR | NONH for all modes of transport |