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. 2015 Aug 10;23(5):406–427. doi: 10.1089/ars.2013.5814

Table 1.

Isoform Selectivity of Novel Catalytic Subunits of Nicotinamide Adenine Dinucleotide Phosphate Oxidases Inhibitors

  IC50 (μM)
Compound NOX1 NOX2 NOX3 NOX4 NOX5 DUOX1 DUOX2 XO/AO
GKT136901 (92, 118) 0.16a,b 1530a,b   0.17a,b 0.45a,b     >30,000b
GKT137831 (5) 0.14a,b 1750a,b   0.11a,b 0.41a,b     >100b
ML171 (58) 0.25c 5.00c 3.00c 5.00c       5.50
VAS2870 (52, 55)   0.77d            
VAS3947 (181) 12.0a 2.00d   13.00a       n.s.e
Celastrol (76) 0.41c 0.59c   2.79c 3.13c     >100
Ebselen (76, 164) 0.15c 0.50c   >50.0c 0.70a     n.s.f
Perhexiline (55, 85)   3.0d           n.s.f
Grindelic acid (89)   >20.0d   2.06c >20.0c     n.s.g
NOX2ds-tat (36) n.s.a,h 0.74a   n.sa,h       n.s.h
NOXA1ds (143) 0.02a n.s.a,h   n.s.a,h n.s.a,h     n.s.h
Fulvene-5 (15)   ∼5.00c   ∼5.00c        
ACD 084 (89)   >5.00c   3.08c >5.00c     n.s.i
Phenantridinones (19)       0.17c       n.s.h
Shionogi (55)   0.56d            
S17834                
Imipramin blue (117)       ∼5.00        

IC50 values of NOX inhibitors for different NOX isoforms and XO or AO activity are presented as determined in different cellular or cell-free assays as described in the respective publication and indicated with the superscription. The IC50 values that suggest relative NOX isoform selectivity are shown in bold. Only some inhibitors were tested for XO inhibition or ROS-scavenging effects, and inhibition was not significant (n.s.) for some of these compounds.

IC50 values were determined in acell-free or lysate assay; bKi were published; coverexpressing cells; dnative cells; eno significant inhibition for concentrations of approximately 30 μM or f100 μM, g20 μM, h10 μM, i5 μM.

AO, antioxidant; DUOX, dual oxidase; IC50, concentration with 50% inhibition of activity; NADPH, nicotinamide adenine dinucleotide phosphate; NOX, catalytic subunit of NADPH oxidases; NOX2ds, NOX2 docking sequence; XO, xanthine oxidase.