A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC50 = 0.129 µM, and 0.25 µM) in human HT29 and HEK293 cell-based assays, respectively. Unlike most other currently used Nox inhibitors, it only has marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms (IC50 = 5 µM, 3 µM and 5 µM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC50 = 5.5 µM) in HEK293 cell-based assays. It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ~ 100 nM; however, its inhibitory effect is reversed through over-expression of Nox1, thereby suggesting that this compound is highly selective for Nox1, with little effect against Nox2-dependent ROS generation (IC50 >10 µM). Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Gianni, D., et al. 2010. ACS Chem. Biol.5, 981.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
