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. Author manuscript; available in PMC: 2012 Jun 1.
Published in final edited form as: Nat Rev Drug Discov. 2011 Jun;10(6):453–471. doi: 10.1038/nrd3403

Table 2.

NADPH oxidase inhibitors

Name Structure Best characterized mechanism of
action relevant to NADPH oxidase		 Other pharmacological effects Refs
AEBSF graphic file with name nihms377394t1.jpg Oxidase assembly inhibitor: inhibits association of NOX2 subunit with p47phox. Does not scavenge O2•− generated in cell-free systems Nonselective serine protease inhibitor 215
Apocynin graphic file with name nihms377394t2.jpg Oxidase assembly inhibitor: inhibits association of p47phox with membrane-bound heterodimer Scavenger of hydrogen peroxide 216−218
DPI graphic file with name nihms377394t3.jpg Flavoprotein inhibitor: abstracts electrons from FAD and prevents electron flow through the flavocytochrome conduit Inhibitor of NADH-ubiquinone oxidoreductase, NADH dehydrogenase, xanthine oxidase, cytochrome p450 oxidoreductase, NOS and bacterial nicotine oxidase 157,158, 219−223
GK-136901 graphic file with name nihms377394t4.jpg Purported NOX1 and NOX4 oxidase inhibitor. Mechanism of action not defined, but structural similarity with NADPH suggests that it may act as a competitive substrate inhibitor of this enzyme None reported 148,224
ML171 graphic file with name nihms377394t5.jpg A phenothiazine compound with selectivity for NOX1 oxidase (IC50 of 0.25 µM) over other NADPH oxidases (IC50 >3 µM). Does not scavenge ROS generated by xanthine oxidase activity None reported 149
Nox2ds-tat [H]-RKKRRQRRRCSTRIRRQL-NH2 Oxidase assembly inhibitor: inhibits association of NOX2 subunit with p47phox. Does not scavenge O2•− generated by cell-free systems None reported 57,188
Plumbagin graphic file with name nihms377394t6.jpg Inhibits NAD(P)H-dependent O2•− production in various cell lines that express NOX4 oxidase; mechanism of action unknown Napthoquinone structure may impart ROS-scavenging effects 225,226
PR-39 RRRPRPPYLPRPRPPPFFPPRLPPRIPPGFPPRFPPRFP Binds to SH3 domains of the p47phox subunit and prevents binding to the p22phox subunit Not selective for NADPH oxidase as it is likely to inhibit other proteins containing SH3 domains 184
S17834 graphic file with name nihms377394t7.jpg Flavonoid derivative proposed to directly inhibit NADPH oxidase activity, although the mechanism of action is undefined None reported 140
VAS2870 graphic file with name nihms377394t8.jpg Undefined mechanism of action; inhibits NADPH oxidase activity in NOX2 oxidase-containing HL-60 cell line and in vascular endothelial cells containing NOX2 and NOX4 oxidases; does not scavenge O2•− None reported 144,145
VAS3947 graphic file with name nihms377394t9.jpg A triazolopyrimidine that reduced NADPH oxidase-derived ROS production in several cell lines with low micromolar potency, irrespective of the specific isoforms expressed; showed no inhibitory effects against xanthine oxidase-derived ROS or eNOS activity None reported 146

eNOS, endothelial nitric oxide synthase; IC50, half-maximal inhibitory concentration; NOX, NADPH oxidase; O2•−, superoxide; ROS, reactive oxygen species; SH3, Src homology 3.