Description

• A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC 50 = 0.129μM, and 0.25μM) 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 (IC 50 = 5μM, 3μM and 5μM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC 50 = 5.5μM) in HEK293 cell-based assays
• It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ∽ 100nM; 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 (IC 50 > 10μM)
• Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.