VAS 2870
VAS 2870 structure
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Common Name | VAS 2870 | ||
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| CAS Number | 722456-31-7 | Molecular Weight | 360.392 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 627.0±65.0 °C at 760 mmHg | |
| Molecular Formula | C18H12N6OS | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 333.0±34.3 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of VAS 2870VAS2870 is a NADPH oxidase (NOX) inhibitor. |
| Name | VAS2870 |
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| Synonym | More Synonyms |
| Description | VAS2870 is a NADPH oxidase (NOX) inhibitor. |
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| Related Catalog | |
| Target |
Target: NADPH oxidase[1] |
| In Vitro | VAS2870 is effective to suppress PDGF-BB-dependent activation of NADPH oxidase and subsequent production of intracellular ROS. Furthermore, VAS2870 suppresses PDGF-BB-dependent chemotaxis, but not DNA synthesis. Preincubation with VAS2870 (10 and 20 μM) completely abolishes PDGF-mediated NADPH oxidase activation and ROS production. Preincubation with VAS2870 (0.1-20 μM) does not affect PDGF-induced cell cycle progression. However, it abolishes PDGF-dependent chemotaxis of VSMC in a concentration-dependent manner (100% inhibition at 10 μM)[1]. VAS2870 inhibits dose-dependently autocrine increase of cell number in FaO rat hepatoma cells, and almost completely blocked ROS production and thymidine incorporation when used at 25 mM. VAS2870 blocks serum-dependent cell growth of FaO rat hepatoma cells. VAS2870 inhibits proliferation of different human hepatocellular carcinoma (HCC) cell lines. VAS2870 pretreatment enhances TGF-b-mediated apoptosis of FaO rat hepatoma cells[2]. |
| Kinase Assay | NADPH oxidase activity is measured by lucigenin-enhanced chemiluminescence in a 50 mM phosphate buffer (buffer A), pH 7.0, containing 1 mM EGTA, protease inhibitors, 150 mM sucrose, 5 μM lucigenin, and 250 μM NADPH as substrate. Quiescent cells are starved by serum deprivation for 24 h and treated as indicated, ished twice with ice-cold phosphate buffered saline (PBS), pH 7.4, and harvested. After low spin centrifugation, the pellet is re-suspended in ice-cold buffer A, lacking lucigenin and substrate. Then, the cells are lysed and total protein concentration is determined using a Bradford assay and adjusted to 1 mg/mL. 100 μL aliquots of the protein sample are measured over 6 min in quadruplicates using NADPH (100 μM) as substrate in a scintillation counter. Data are collected at 2 min intervals in order to measure relative changes in NADPH oxidase activity[1]. |
| Cell Assay | To test autocrine growth, cells are serum deprived at 40% confluence and, when indicated, the NADPH oxidase inhibitors Apocynin (300 mM) or VAS2870 are added 30 min before serum deprivation and maintained along the experiment. For TGF-b experiments, cells at 70% confluence are serum deprived for 16 h and treated with 2 ng/mL TGF-β in the presence or absence of the EGFR inhibitor AG1478 (20 mM) or VAS2870 (25 mM), which are added 30 min prior to TGF-β[2]. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 627.0±65.0 °C at 760 mmHg |
| Molecular Formula | C18H12N6OS |
| Molecular Weight | 360.392 |
| Flash Point | 333.0±34.3 °C |
| Exact Mass | 360.079315 |
| LogP | 3.61 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.808 |
| InChIKey | HZSOKHVVANONPV-UHFFFAOYSA-N |
| SMILES | c1ccc(Cn2nnc3c(Sc4nc5ccccc5o4)ncnc32)cc1 |
| Storage condition | 2-8℃ |
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Sex differences in the role of NADPH oxidases in endothelium-dependent vasorelaxation in porcine isolated coronary arteries.
Vascul. Pharmacol. 72 , 83-92, (2015) The present study examined whether vascular function, expression and activity of NADPH oxidases differ between sexes in porcine isolated coronary arteries (PCAs) using selective Nox inhibitors, ML-171... |
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Nox1 upregulates the function of vascular T-type calcium channels following chronic nitric oxide deficit.
Pflugers Arch. 467(4) , 727-35, (2015) Cardiovascular disease is characterised by reduced nitric oxide bioavailability resulting from oxidative stress. Our previous studies have shown that nitric oxide deficit per se increases the contribu... |
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Graviola inhibits hypoxia-induced NADPH oxidase activity in prostate cancer cells reducing their proliferation and clonogenicity.
Sci. Rep. 6 , 23135, (2016) Prostate cancer (PCa) is the leading malignancy among men. Importantly, this disease is mostly diagnosed at early stages offering a unique chemoprevention opportunity. Therefore, there is an urgent ne... |
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