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.
体外研究
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.
BRD7389 (0.85-6.8μM) significantly up-regulates Pdx1 mRNA expression in mouse α-cell line.
BRD7389 also increases β-cell-specific gene expression in primary human islet cells.
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.
RT-PCR
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
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.
分子式
C24H18N2O2
分子量
366.41
CAS号
376382-11-5
运输条件
Room temperature in continental US; may vary elsewhere.