NSC117079-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC117079Cat. No.: HY-19819CAS No.: 500363-63-3分式: CHNOS分量: 473.48作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (316.80 mM)* means soluble, but saturation

2、unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1120 mL 10.5601 mL 21.1202 mL5 mM 0.4224 mL 2.1120 mL 4.2240 mL10 mM 0.2112 mL 1.0560 mL 2.1120 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NSC117079是新型的 PHLPP 抑制剂。IC50 & Target PHLPP 1体外研究NSC-117079 at 30 M induce

3、s neutrophil adhesion to plated fibrinogen from 9.02.4% to 27.08.0% andenhanced neutrophil adhesion caused by 50 ng/mL GM-CSF from 22.96.0% to 47.610.9%. Neutrophil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEadhesion is followed by neutrophil transendothelial migration. Results suggest that PHL

4、PP inhibitor NSC-117079 is effective in preventing Akt from dephosphorylation in neutrophils, and Akt phosphatase PHLPPserves to attenuate neutrophil adhesion but not migration 2.体内研究 A single intraarticular injection of the Phlpp inhibitor NSC117079 attenuates mechanical allodynia and slowsarticula

5、r cartilage degradation in joints with a destabilized meniscus. Animals treated with the Phlpp inhibitorseven weeks after injury maintain normal activity levels, while those in the control group travel shorterdistances and are less active three months after the joint injury. NSC117079 also increases

6、 production ofcartilage extracellular matrix components (glycosaminoglycans and aggrecan) in over 90% of human articularcartilage explants from osteoarthritis patients and increased phosphorylation of Phlpp1 substrates (AKT2,ERK1/2 and PKC) in human articular chondrocytes 1.PROTOCOLAnimal Mice 1Admi

7、nistration 1 Posttraumatic osteoarthritis is induced in male C57Bl/6 mice by surgically destabilizing the meniscus. Sevenweeks after surgery, mice receive a single intra-articular injection of the PHLPP inhibitor NSC117079 (8 M)or saline. Mechanical allodynia is measured with von Frey assays, mobili

8、ty is tracked in an open field system,and cartilage damage is assessed histologically 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jackson TC, et al. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein

9、phosphatase is neuroprotective:differential effects on astrocytes. J Pharmacol Exp Ther. 2013 Nov;347(2):516-28.2. Zhu X, et al. Regulation Of Neutrophil Adhesion And Migration By Ph Domain And Leucine Rich Repeat Protein Phosphatase. A35RECENT ADVANCES IN PHAGOCYTE BIOLOGY / Thematic Poster Session / Sunday, May 20/8:15 AM-4:30 PM / Area G (Hall D, NorthBuilding, Lower Level), Moscone CenterMcePdfHeightCaution: Product has not been fully validated for