TABLE 4.
IC50 values for selected positive hits, determined by monitoring the effect of the compounds on the rate of oxidation of coumarin boronic acid (100 μm) as a probe for H2O2
Differentiated HL60 cells were stimulated with PMA (1 μm) to induce Nox2 activity in HBSS supplemented with HEPES buffer (25 mm) and dtpa (0.1 mm) and the extent of probe oxidation was monitored in 384-well plates using fluorescence plate reader.
| No. | Compound | IC50 (μm) |
|
|---|---|---|---|
| Mean | S.D. | ||
| 1 | Amiodarone·HCl | 11 | 2 |
| 2 | Amoxapine | 16 | 4 |
| 3 | Benzbromarone | 13 | 1.5 |
| 4 | Benzethonium chloride | 23 | 0.7 |
| 5 | Cetylpyridinium chloride | 2.3 | 0.3 |
| 6 | Chlorpromazine·HCl | 13 | 0.6 |
| 7 | Clotrimazole | 59 | 25 |
| 8 | Diphenyleneiodonium | 0.08 | 0.07 |
| 9 | Dyclonine | 39 | 16 |
| 10 | Econazole nitrate | 22 | 1.1 |
| 11 | Hexachlorophene | 2.2 | 0.4 |
| 12 | Mefloquine·HCl | 16 | 0.4 |
| 13 | Miconazole | 15 | 6.5 |
| 14 | Mitoxantrone | 18 | 12 |
| 15 | Phenylarsine oxide | 0.2 | 0.04 |
| 16 | Promazine·HCl | 31 | 1.6 |
| 17 | Sulconazole nitrate | 19 | 2.6 |
| 18 | Suloctidil | 7.7 | 3.5 |
| 19 | Tamoxifen citrate | 18 | 0.5 |
| 20 | Thimerosal | 2.2 | 0.6 |
| 21 | Thioridazine | 9.3 | 2.1 |
| 22 | Tioconazole | 9.2 | 0 |
| 23 | Trifluoperazine | 9 | 2.2 |
| 24 | Triflupromazine·HCl | 12 | 2.6 |