Table 4.
Isoform specificity of selected peptides and small molecule inhibitors of NADPH oxidase.
| Name | Structure | IC50s (μM) (* = Ki in μM) | Suggested Mechanism of Inhibition | Ref. | |||||
|---|---|---|---|---|---|---|---|---|---|
| NOX1 | NOX2 | NOX3 | NOX4 | NOX5 | XO | ||||
| DPI |
|
0.2 | 0.1 | 0.1 | 0.02 | yes | FAD site | (1237) | |
| AEBSF |
|
(1245) | |||||||
| VAS2870 |
|
↓ |
10.6
(Neutrophils) 2 (HL-60) |
↓ | (1335–1337) | ||||
| VAS3947 |
|
↓ |
1–2
(HL-60 cells) |
↓ | ns | (1336) | |||
| APX-115 (Isuzinaxib) |
|
1.08 | 0.57 | 0.63 | (720, 1251, 1338) | ||||
| Celastrol |
|
0.41 | 0.59 | 2.7 | 3.13 | ns | p47phox-p22phox interface | (1252) | |
| Setanaxib(aka GKT137831/GKT-831) |
|
0.11 | 1.75 | 0.14 | 0.41 | >30 * | (655, 1339) | ||
| GKT 136901 |
|
0.160 * | 1.530 * | 0.17 * | 0.45 | >30 * | (437, 1255) | ||
| GKT-771(aka GKT310771) | Not disclosed | 0.065(ki) | Inactive | Inactive | 4.3(ki) | Inactive | (1103) | ||
| ML171 |
|
0.25 | 5.00 | 5.00 | 5.50 | (1260) | |||
| NOS31 |
|
(401) | |||||||
| NoxA1ds | EPVDALGKAKV | 0.02 | ns | ns | ns | ns | Nox1-NoxA1 interface | (439) | |
| Nox2ds-tat | RKKRRQRRRCSTRIRRQL | ns | 0.74 | ns | ns | ns | Nox2(B-loop)-p47 phox | (57, 740) | |
| GSK2795039 |
|
>100 | <2.88 | >100 | >100 | >100 | XO(29) | (1269) | |
| Ebselen |
|
0.15 | 0.5 | ns | 0.7 | ns | p47phox and p67phox translocation | (1340) | |
| ML090 |
|
0.025 | Inactive | 0.02 | 0.01 | (1341, 1342) | |||
| CPP11G |
|
ns | 20 | ns | ns | ns | p47phox-p22phox interface | (1070, 1071) | |
| CPP11H |
|
ns | 32 | ns | ns | ns | p47phox-p22phox interface | (1070, 1071) | |
| CYR5099 |
|
Inactive | 2.8–5.2 | (628) | |||||
| PHOX-I1 |
|
ND | 3 | Inactive | Rac1/2-p67 phox | (1274) | |||
| PHOX-I2 |
|
ND | 1 | Inactive | Rac1/2-p67 phox | (1274) | |||
| Naloxone |
|
2 | p47phox binding | (1279) | |||||
| NCATS-SM7270 |
|
(1280) | |||||||
| GLX351322 |
|
40 | 5 | (1289) | |||||
| GLX481372 |
|
7 | 16 | 3.2 | 0.68 | 0.57 | (1290) | ||
| GLX7013114 | Not disclosed | Inactive | Inactive | Inactive | 0.3 | Inactive | (1290) | ||
| GLX481304 |
|
Inactive | 1.25 | Inactive | 1.25 | Inactive | (1290, 1291) | ||
| Grindelic Acid (ACD042) |
|
>20 | 2.06 | (1292) | |||||
| ACD 084 |
|
>5.00 | 3.08 | >5.00 | (1292) | ||||
| ML090 |
|
0.025 | Inactive | 0.02 | 0.01 | (1341, 1342) | |||
| Gedunin |
|
Hsp90 site | (1296) | ||||||
| Comp10 |
|
ND | 3.3 | 95 | p47phox-p22phox interface | (1284) | |||
| Comp33 |
|
ND | 12 | 94 | p47phox-p22phox interface | (1284) | |||
(↓= inhibits but no IC50 determined; ns= not significant; blank space=not determined;
*
= Ki)