| Name | bas 05532738 |
|---|---|
| Synonyms |
BRD7389,cancer,S6K,Inhibitor,BRD 7389,colon,inhibit,RSK,islets,diabetes,BRD-7389,pancreatic,SNU-407,Ribosomal S6 Kinase (RSK)
1-(Phenethylamino)-2H-naphtho[1,2,3-de]quinoline-2,7(3H)-dione 1-[(2-Phenylethyl)amino]-3H-naphtho[1,2,3-de]quinoline-2,7-dione BRD-7389, p90 ribosomal S6 kinase RSK inhibitor BRD 7389 (BRD7389) 1-Phenethylamino-3H-naphtho[1,2,3-de]quinoline-2,7-dione 1-[(2-Phenylethyl)amino]-naphtho-3H-[1,2,3-de]quinoline-2,7-dione BRD7389, 10 mM in DMSO 3H-Naphtho[1,2,3-de]quinoline-2,7-dione, 1-[(2-phenylethyl)amino] Insulin Expression Inducer, BRD7389 - - Calbiochem BRD7389 >= (HPLC) hms1493i11 Insulin Expression Inducer, BRD7389 |
| 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]. |
|---|---|
| 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 |
|---|---|
| Molecular Weight | 366.41200 |
| Exact Mass | 366.13700 |
| PSA | 62.22000 |
| LogP | 4.87940 |
| Hazard Statements | H413 |
|---|---|
| RIDADR | NONH for all modes of transport |