Table 1. Re-screening data on potential agonists or antagonists identified in the initial chemical screen.
Small molecules that were identified as potential regulators in the screen were retested in duplicate at the original concentration screened (Concentration #1) and two dilutions (Concentrations #2 and #3) for their effects on Hepcidin-luciferase activity, measured as fold-change over the activity from cells treated with DMSO only. Candidate regulators that increased mean Hepcidin-luciferase activity at least 2-fold at the original concentration were considered agonists (shaded in green), while candidate regulators that decreased mean Hepcidin-luciferase activity at least 2-fold were considered antagonists (shaded in orange).
| Regulator Name | Concentration #1 (μM) | Hepcidin-Luciferase Activity at Conc. #1 Mean±SE (AU) N=2 | Concentration #2 (μM) | Hepcidin-Luciferase Activity at Conc. #2 Mean±SE (AU) N=2 | Concentration #3 (μM) | Hepcidin-Luciferase Activity at Conc. #3 Mean±SE (AU) N=2 |
|---|---|---|---|---|---|---|
| POTENTIAL AGONISTS | ||||||
| Vorinostat | 33 | 56.08±35.27 | 6.6 | 48.14±6.70 | 1.3 | 14.60±4.68 |
| 9-aminoacridine | 33 | 49.76±12.27 | 6.6 | 1.14±0.40 | 1.3 | 0.68±0.07 |
| Acrisorcin | 33 | 29.85±1.50 | 6.6 | 0.99±0.06 | 1.3 | 0.77±0.00 |
| Ethacridine lactate | 33 | 15.18±1.13 | 6.6 | 1.35±0.24 | 1.3 | 1.12±0.18 |
| Doxorubicin | 12 | 11.39±0.49 | 2.4 | 0.68±0.06 | 0.5 | 0.77±0.02 |
| Daunorubicin | 12 | 11.33±0.07 | 2.4 | 0.99±0.05 | 0.5 | 0.67±0.05 |
| Leflunomide | 33 | 5.50±0.29 | 6.6 | 3.10±0.23 | 1.3 | 1.12±0.18 |
| #5322770 | 66 | 5.03±0.21 | 12.2 | 1.42±0.04 | 2.6 | 0.84±0.06 |
| Ipriflavone | 33 | 4.57±0.30 | 6.6 | 3.41±0.08 | 1.3 | 2.56±0.07 |
| Lansoprazole | 33 | 4.09±0.44 | 6.6 | 0.98±0.01 | 1.3 | 0.58±0.01 |
| Pterostilbene | 33 | 4.06±0.59 | 16.5 | 3.91±0.28 | 8.25 | 2.21±0.19 |
| Amlexanox | 33 | 3.84±0.95 | 6.6 | 2.65±0.06 | 1.3 | 0.67±0.02 |
| Nabumetone | 33 | 3.74±0.19 | 16.5 | 3.16±0.30 | 8.25 | 3.61±0.95 |
| Topotecan | 33 | 3.63±1.39 | 6.6 | 0.57±0.05 | 1.3 | 0.73±0.04 |
| Camptothecin | 33 | 3.62±0.62 | 6.6 | 1.55±0.34 | 1.3 | 0.60±0.05 |
| Chrysin | 26 | 3.53±0.60 | 5.2 | 1.09±0.11 | 1.0 | 0.76±0.01 |
| GTP-14564 | 11 | 3.07±0.60 | 2.2 | 1.35±0.07 | 0.4 | 1.17±0.15 |
| 10058-F4 | 33 | 2.92±0.23 | 6.6 | 2.17±0.01 | 1.3 | 1.25±0.13 |
| SB 204741 | 33 | 2.87±0.22 | 6.6 | 1.96±0.18 | 1.3 | 1.09±0.04 |
| Phenazopyridine | 26 | 2.85±0.04 | 5.2 | 1.51±0.08 | 1.0 | 0.95±0.12 |
| AS-252424 | 33 | 2.84±0.02 | 6.6 | 1.40±0.03 | 1.3 | 0.73±0.02 |
| AG 1296 | 11 | 2.41±0.14 | 2.2 | 1.03±0.11 | 0.4 | 0.90±0.07 |
| SP 600125 | 33 | 1.86±0.00 | 6.6 | 1.11±0.02 | 1.3 | 0.93±0.09 |
| Fenbendazole | 22 | 1.75±0.08 | 4.4 | 1.03±0.20 | 0.9 | 0.96±0.12 |
| #5105276 | 66 | 1.73±0.04 | 12.2 | 0.75±0.13 | 2.6 | 0.74±0.02 |
| GW9662 | 33 | 1.66±0.08 | 6.6 | 1.12±0.05 | 1.3 | 1.09±0.01 |
| #5102420 | 66 | 1.66±0.06 | 12.2 | 0.80±0.11 | 2.6 | 0.83±0.16 |
| Imatinib | 33 | 1.24±0.13 | 16.5 | 1.18±0.06 | 8.25 | 1.31±0.06 |
| Nocodazole | 22 | 1.13±0.02 | 4.4 | 0.84±0.11 | 0.9 | 0.84±0.01 |
| #5193825 | 66 | 1.13±0.14 | 12.2 | 0.67±0.01 | 2.6 | 0.69±0.06 |
| POTENTIAL ANTAGONISTS | ||||||
| #5215082 | 66 | 1.09±0.08 | 12.2 | 0.87±0.04 | 2.6 | 0.79±0.02 |
| #5146972 | 66 | 1.08±0.00 | 12.2 | 0.72±0.05 | 2.6 | 0.66±0.03 |
| SU-6668 | 33 | 0.31±0.02 | 6.6 | 0.67±0.09 | 1.3 | 0.88±0.01 |