BRD 7389

BRD 7389

Catalog Number:
L002372722APE
Mfr. No.:
APE-B9012
Price:
$273
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      • Overview
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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]

          [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.

      • Properties
        • Alternative Name
          2-hydroxy-1-(phenethylamino)-7H-naphtho[1,2,3-de]quinolin-7-one
          CAS Number
          376382-11-5
          Molecular Formula
          C24H18N2O2
          Molecular Weight
          366.41
          Appearance
          Brown solid
          Purity
          Purity ≥95.00%
          Solubility
          Soluble in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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