| Bioactivity | VAS2870 is a NADPH oxidase (NOX) inhibitor. | ||||||||||||
| Target | Target: NADPH oxidase | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | VAS2870 | ||||||||||||
| CAS | 722456-31-7 | ||||||||||||
| Formula | C18H12N6OS | ||||||||||||
| Molar Mass | 360.39 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. 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-β-induced apoptosis of liver tumor cells. Biochem Pharmacol. 2011 Apr 1;81(7):917-24. |