Drug intelligence / Profile preview

diphenyleneiodonium

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Diphenyleneiodonium is a synthetic small molecule best known as a potent inhibitor of NADPH oxidase enzymes, particularly NADPH oxidase 2 (NOX2). It also inhibits other flavoprotein-containing enzymes such as nitric oxide synthases (NOS) and NADPH cytochrome P450 oxidoreductase. Diphenyleneiodonium has been used experimentally to study the role of reactive oxygen species (ROS) in biological systems and exhibits antimicrobial activity against non-tuberculous mycobacteria. Its mechanism involves irreversible inhibition by binding to the flavin cofactor site of target enzymes, thereby blocking electron transfer and enzyme activity[1][3][5][8]. The compound is primarily used in research settings; it does not have approved clinical indications.

Other names
dibenziodoliumdiphenylene iodonium2,2'-biphenylyleneiodonium
02

Targets

AcetylcholinesteraseButyrylcholinesterasePOR (NADPH-cytochrome P450 oxidoreductase)NOX2 (NADPH oxidase 2)NOS1 (nNOS)

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