Table 1.
Mechanistic activity and specificity validation of selected catalytic subunits of nicotinamide adenine dinucleotide phosphate oxidase inhibitors [17,154,155]. XO: Xanthine Oxidase, eNOS: endothelial nitric oxide synthase, GPCR: G-protein coupled receptor.
| Compound | Direct Interaction with NOX Complex | Off Target Effects |
|---|---|---|
| GKT136901 | Yes (Cell free assays and in vivo) | Yes (XO) |
| GKT137831 | Yes (Cell free assays and in vivo) | Yes (XO, eNOS) |
| ML171 | n.a. | Yes, minor (5-HT2b receptor) |
| VAS2870 | Inhibits NOX activity when added before the complex assembly | XO |
| VAS3947 | Yes (Cell free assays) | |
| Celastrol | Yes (Cell free assays) | XO |
| Ebselen | Inhibits NOX activity when added before the complex assembly | XO |
| Perhexiline | Yes (Cell free assays) | |
| ACD084 | Yes (Cell free assays) | Mitochondrial complex I |
| NOX2ds-tat | Inhibits NOX activity when added before the complex assembly | XO |
| NOXA1ds | Inhibits NOX activity when added before the complex assembly | XO |