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  • BRD 7389
BRD 7389的可视化放大

BRD 7389

An inhibitor of RSKs

原价
¥562-2987
价格
450-2390
BRD 7389的二维码

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  • 货号: ajci17800
  • CAS: 376382-11-5
  • 别名:
  • 分子式: C24H18N2O2
  • 分子量: 366.41
  • 纯度: >98%
  • 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
  • 储存: 4°C, protect from light
  • 库存: 现货

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]

参考文献:
[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.

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