Description
Diphenyleneiodonium (DPI) is an inhibitor of NADPH oxidase (NOX; EC
50 = 0.1 μM in HeLa cells). It also inhibits nitric oxide synthase (NOS; IC
50 = 0.05 μM in isolated mouse peritoneal macrophages). DPI (10, 50, and 100 μM) induces the production of reactive oxygen species (ROS) in, and apoptosis of, human umbilical vein endothelial cells (HUVECs). It inhibits NETosis induced by phorbol 12-myristate 13-acetate (PMA; ) in isolated human neutrophils when used at a concentration of 10 μM. DPI (2 mg/kg) reduces tumor growth in HT-29 and LS 174T colon cancer mouse xenograft models.
Chemical Properties
Crystalline Solid
Uses
Diphenyleneiodonium Chloride binds strongly to flavoproteins and thus inhibits NO synthase, NADG reductase and NADPH oxidase.Diphenyleneiodonium Chloride solubility: 5 mg in 1.7 mL of H2O:DMSO 40:60; 10 mg in 1.1 mL H2O:DMSO 10:90
Uses
Binds strongly to flavoproteins and thus inhibits NO synthase, NADG reductase and NADPH oxidase.
Solubility: 5 mg in 1.7 mL of H2O:DMSO 40:60; 10 mg in 1.1 mL H2O:DMSO 10:90
Definition
ChEBI: An organic chloride salt having dibenziodolium as the counterion.
Biochem/physiol Actions
A potent and reversible inhibitor of nitric oxide synthetase from macrophages and endothelial cells. Also inhibits other flavoenzymes such as neutrophil NADPH oxidase.
storage
Desiccate at -20°C
References
[1] DENNIS J. STUEHR. Inhibition of macrophage and endothelial cell nitric oxide synthase by diphenyleneiodonium and its analogs1[J]. FASEB Journal, 1991, 5 1: 98-103. DOI:
10.1096/fasebj.5.1.1703974[2] C M YEA O T J A R Cross. Purification and some properties of the 45 kDa diphenylene iodonium-binding flavoprotein of neutrophil NADPH oxidase.[J]. Biochemical Journal, 1990, 265 1: 95-100. DOI:
10.1042/bj2650095[3] CHENLI YE. Identification of a novel small-molecule agonist for human G protein-coupled receptor 3.[J]. Journal of Pharmacology and Experimental Therapeutics, 2014, 349 3: 437-443. DOI:
10.1124/jpet.114.213082[4] Diphenyleneiodonium inhibits NF-kappaB activation and iNOS expression induced by IL-1beta: involvement of reactive oxygen species
[5] H. KONO. Diphenyleneiodonium sulfate, an NADPH oxidase inhibitor, prevents early alcohol-induced liver injury in the rat.[J]. American journal of physiology. Gastrointestinal and liver physiology, 2001, 73 1: G1005-12. DOI:
10.1152/ajpgi.2001.280.5.g1005
