VAS2870 - NADPH Oxidase 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVAS2870Cat. No.: HY-12804CAS No.: 722456-31-7分式: CHNOS分量: 360.39作靶點: NADPH Oxidase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 83.3 mg/mL (231.14 mM; Need u

2、ltrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7748 mL 13.8739 mL 27.7477 mL5 mM 0.5550 mL 2.7748 mL 5.5495 mL10 mM 0.2775 mL 1.3874 mL 2.7748 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件

3、，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.94 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.94 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 VAS2870是NA

4、DPH氧化酶 (NADPH oxidase (NOX) 抑制劑。IC50 & Target Target: NADPH oxidase 1體外研究 VAS2870 is effective to suppress PDGF-BB-dependent activation of NADPH oxidase and subsequentproduction of intracellular ROS. Furthermore, VAS2870 suppresses PDGF-BB-dependent chemotaxis, butnot DNA synthesis. Preincubation wi

5、th VAS2870 (10 and 20 M) completely abolishes PDGF-mediatedNADPH oxidase activation and ROS production. Preincubation with VAS2870 (0.1-20 M) does not affectPDGF-induced cell cycle progression. However, it abolishes PDGF-dependent chemotaxis of VSMC in aconcentration-dependent manner (100% inhibitio

6、n at 10 M) 1. VAS2870 inhibits dose-dependentlyautocrine increase of cell number in FaO rat hepatoma cells, and almost completely blocked ROS productionand thymidine incorporation when used at 25 mM. VAS2870 blocks serum-dependent cell growth of FaO rathepatoma cells. VAS2870 inhibits proliferation

7、of different human hepatocellular carcinoma (HCC) cell lines.VAS2870 pretreatment enhances TGF-b-mediated apoptosis of FaO rat hepatoma cells 2.PROTOCOLKinase Assay 1 NADPH oxidase activity is measured by lucigenin-enhanced chemiluminescence in a 50 mM phosphatebuffer (buffer A), pH 7.0, containing

8、1 mM EGTA, protease inhibitors, 150 mM sucrose, 5 M lucigenin, and250 M NADPH as substrate. Quiescent cells are starved by serum deprivation for 24 h and treated asindicated, ished twice with ice-cold phosphate buffered saline (PBS), pH 7.4, and harvested. After low spincentrifugation, the pellet is

9、 re-suspended in ice-cold buffer A, lacking lucigenin and substrate. Then, the cellsare lysed and total protein concentration is determined using a Bradford assay and adjusted to 1 mg/mL. 100L aliquots of the protein sample are measured over 6 min in quadruplicates using NADPH (100 M) assubstrate in

10、 a scintillation counter. Data are collected at 2 min intervals in order to measure relative changesin NADPH oxidase activity 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 To test autocrine growth, cells are serum deprived at 40% conflu

11、ence and, when indicated, the NADPHoxidase inhibitors Apocynin (300 mM) or VAS2870 are added 30 min before serum deprivation andmaintained along the experiment. For TGF-b experiments, cells at 70% confluence are serum deprived for 16h and treated with 2 ng/mL TGF- in the presence or absence of the E

12、GFR inhibitor AG1478 (20 mM) orVAS2870 (25 mM), which are added 30 min prior to TGF- 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. ten Freyhaus H, et al. Novel Nox inhibitor VAS2870 attenuates PDGF-dependent smooth muscle cell chemotaxis, but not proliferation.Cardiovasc Res. 2006 Jul 15;71(2):331-41.2. Sancho P, et al. The NADPH oxidase inhibitor VAS2870 impairs cell growth and enhances TGF-induced apoptosis of liver tumor cells.Biochem Pharmacol. 2011 Apr 1;81(7):917-24.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.Med