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BRD 7389

In stock
Catalog No.
B9012
P90 RSK inhibitor
Grouped product items
SizePriceStock Qty
5mg
$94.00
In stock
10mg
$172.00
In stock

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Email: [email protected]

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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

Physical AppearanceBrown solid
StorageStore at -20°C
M.Wt366.41
Cas No.376382-11-5
FormulaC24H18N2O2
SolubilitySoluble in DMSO
Chemical Name2-hydroxy-1-(phenethylamino)-7H-naphtho[1,2,3-de]quinolin-7-one
SDFDownload SDF
Canonical SMILESO=C1C2=CC=CC=C2C3=C(NCCC4=CC=CC=C4)C(O)=NC5=CC=CC1=C53
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

BRD 7389