BRD7389

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BRD7389 

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。

BRD7389

BRD7389 Chemical Structure

CAS No. : 376382-11-5

规格 价格 是否有货
10 mg ￥7200 询问价格 & 货期

* Please select Quantity before adding items.

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[1].

IC50 & Target[1]

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
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

366.41

Formula

C24H18N2O2
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)
参考文献

  • [1]. Fomina-Yadlin D, et al. Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.

    [2]. Park YS, et al. EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-407 colon cancer cells by muscarinic acetylcholine receptors. Mol Cell Biochem. 2012 Nov;370(1-2):191-8.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务