BRD7389
目录号 : KM2843 CAS No. : 376382-11-5 纯度 : 98%

BRD7389 是一种特异性的 RSK 家族激酶抑制剂,对 RSK1,RSK2 和 RSK3 的 IC50 分别为 1.5 μM,2.4 μM 和 1.2 μM。BRD7389 可以诱导胰腺 α 细胞中胰岛素表达。

规格 价格 是否有货 数量
10mg
In-stock
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生物活性

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.

IC50&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)

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.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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