BRD 7389
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.
Physical Appearance | Brown solid |
Storage | Store at -20°C |
M.Wt | 366.41 |
Cas No. | 376382-11-5 |
Formula | C24H18N2O2 |
Solubility | Soluble in DMSO |
Chemical Name | 2-hydroxy-1-(phenethylamino)-7H-naphtho[1,2,3-de]quinolin-7-one |
SDF | Download SDF |
Canonical SMILES | O=C1C2=CC=CC=C2C3=C(NCCC4=CC=CC=C4)C(O)=NC5=CC=CC1=C53 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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