BRD 7389 |
| Catalog No.GC16779 |
BRD 7389 est un inhibiteur spécifique de la famille des kinases RSK avec des IC50 de 1,5 μM, 2,4 μM et 1,2 μM pour RSK1, RSK2 et RSK3, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 376382-11-5
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| Solubility | 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. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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