2-Acetylphenothiazine

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.¹ It does not affect xanthine oxidase-dependent or mitochondrial ROS generation.¹ 2-APT prevents ROS-dependent formation of ECM-degrading invadopodia in colon cancer cells.¹ It also abolishes collagen-induced superoxide production by platelets (IC₅₀ = 306 nM), preventing platelet aggregation and thrombus formation.² 2-APT protects beta cells from cytokine-induced apoptosis by inhibiting NOX1.³ 2-APT can also activate the human transient receptor potential ankyrin 1 (TRPA1) nociceptor at 1-30 µM.⁴

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1. Gianni, D., Taulet, N., Zhang, H., et al. A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells. ACS Chem. Biol. 5(10), 981-993 (2010).

2. Vara, S., Campanella, M., and Pula, G. The novel NOX inhibitor 2-acetylphenothiazine impairs collagen-dependent thrombus formation in a GPVI-dependent manner. Br. J. Pharmacol. 168(1), 212-224 (2013).

3. Weaver, J.R., Grzesik, W., and Taylor-Fishwick, D.A. Inhibition of NADPH oxidase-1 preserves β cell function. Diabetologia 58(1), 113-121 (2015).

4. Suzuki, H., Hatano, N., Muraki, Y., et al. The NADPH oxidase inhibitor diphenyleneiodonium activates the human TRPA1 nociceptor. Am. J. Physiol. Cell Physiol. 307(4), C384-C394 (2014).