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BRD 7389

カタログ番号GC16779

BRD 7389 は、RSK1、RSK2、および RSK3 に対してそれぞれ 1.5 μM、2.4 μM、および 1.2 μM の IC50 を持つ特定の RSK ファミリー キナーゼ阻害剤です。

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BRD 7389 化学構造

Cas No.: 376382-11-5

サイズ 価格 在庫数 個数
1mg
$46.00
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5mg
$135.00
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10mg
$247.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BRD7389 is a Rsk family kinase inhibitor. [1]

Rsk has been suggested to phosphorylate a large number of cellular substrates and plays an important role in promoting cell growth and survival. Knockdown of Rsk family members would have an effect on insulin production inα-cells. Increasing in insulin expression upon RNAi of individual Rsk proteins can be observed, but the effect is not as strong as compound treatment with BRD7389.[1]

BRD7389 functions by inhibiting multiple Rsk family members simultaneously. BRD7389 also increases β-cell–specific gene expression in primary human islet cells. Assay-performance profile analysis suggests biochemical and cellular inhibition of the Rsk kinase family by BRD7389 is likely related to its ability induce a β-cell-like state. [2]

Treatment of TC1 cells with BRD7389 led to a decrease in the overall glycolytic activity and mitochondrial respiration rates, a phenotype reminiscent of the beta cell line. BRD7389 also increases the endocrine cell content and function of donor human pancreatic islets in culture.[2,3]

References:
[1]Sapkota GP, Cummings L, Newell FS,etal. , BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38.
[2]Choudhary A, Hu He K, Mertins P, etal. , Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming. PLoS One. 2014 Apr 23;9(4):e95194.
[3]Fomina-Yadlin D, Kubicek S, Walpita D,etal. , Small-molecule inducers of insulin expression in pancreatic alpha-cells. Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15099-104.

Chemical Properties

Cas No. 376382-11-5 SDF
Chemical Name 2-hydroxy-1-(phenethylamino)-7H-naphtho[1,2,3-de]quinolin-7-one
Canonical SMILES O=C1C2=CC=CC=C2C3=C(NCCC4=CC=CC=C4)C(O)=NC5=CC=CC1=C53
Formula C24H18N2O2 M.Wt 366.41
溶解度 DMF: 20 mg/mL,DMF:PBS (pH 7.2)(1:3): 0.25 mg/mL,DMSO: 12.5 mg/mL,Ethanol: slightly soluble Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.7292 mL 13.6459 mL 27.2918 mL
5 mM 0.5458 mL 2.7292 mL 5.4584 mL
10 mM 0.2729 mL 1.3646 mL 2.7292 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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