2-Acetylphenothiazine (2-APT) is a selective, cell-active inhibitor of NADPH oxidase 1 (NOX1) that blocks the generation of reactive oxygen species (ROS) in HT-29 cells with an IC50 value of 0.129 μM. It does not affect xanthine oxidase-dependent or mitochondrial ROS generation. 2-APT prevents ROS-dependent formation of ECM-degrading invadopodia in colon cancer cells. It also abolishes collagen-induced superoxide production by platelets (IC50 = 306 nM), preventing platelet aggregation and thrombus formation. 2-APT protects beta cells from cytokine-induced apoptosis by inhibiting NOX1. 2-APT can also activate the human transient receptor potential ankyrin 1 (TRPA1) nociceptor at 1-30 μM.
Yellow white or green crystalline powder
2-Acetylphenothiazine is a potent and selective NADPH oxidase 1 (NOX1) inhibitor that blocks NOX1-dependent ROS generation. 2-Acetylphenothiazine has been shown to inhibit SrcYF-induced invadopodia formation in human DLD1 colon cancer cells.
2-Acetylphenothiazine was used as a NADPH oxidase (NOX) inhibitor in human platelet functional responses and intracellular signaling pathways. It was also used in the synthesis of 2-phenothiazin-2′-yl-cinchoninic acid derivatives.
ChEBI: 1-(10H-phenothiazin-2-yl)ethanone is a member of phenothiazines.
