Table 2.
List of potential hit compounds identified by the primary screening, and effect of the same compounds on GYY4137-induced fluorescence responses. Compounds were screened at 30 μM (except for compounds indicated by asterisk, where testing was conducted at the indicated concentration) against CBS-induced AzMC fluorescence and re-tested at 30 μM (except for compounds indicated by asterisk, where testing was conducted at the indicated concentration) against CBS- and GYY4137-induced AzMC fluorescence. Data are shown as mean ± SEM, n = 3.
| Potential hit compound | Library | Initial screen (% inhibition of CBS-induced AzMC fluorescence) | Confirmation (% inhibition of CBS-induced AzMC fluorescence) | Confirmation (% inhibition of GYY4137-induced AzMC fluorescence) |
|---|---|---|---|---|
| 5-(N,N-hexamethylene)amiloride | LOPAC | 72% | 58 ± 3 | 54 ± 4 |
| Ruthenium red | LOPAC | 72% | 72 ± 6 | 72 ± 3 |
| NSC 95397 (2,3bis[(2-Hydroxyethyl)thio]-1,4-naphthoquinone) | LOPAC | 70% | 59 ± 8 | 58 ± 1 |
| O-(Carboxymethyl)hydroxylamine hemihydrochloride (AOAA) | LOPAC | 70% | 89 ± 1 | 2 ± 1 |
| Aurintricarboxylic acid | LOPAC | 59% | 87 ± 1 | −2 ± 1 |
| Benserazide hydrochloride | LOPAC | 49% | 44 ± 1 | 4 ± 2 |
| Tyrphostin AG 537 | LOPAC | 49% | 42 ± 1 | 48 ± 2 |
| 2,3-Dimethoxy-1,4-naphthoquinone | LOPAC | 49% | 53 ± 1 | 51 ± 4 |
| Closantel | FDA | 43% | 25 ± 5 | 31 ± 2 |
| Progesterone | IDC | 68% | 75 ± 3 | 64 ± 1 |
| Nifuroxazide | IDC | 48% | 55 ± 4 | 50 ± 2 |
| Chlorophyllide cu complex Na salt | Killer | 82% | 97 ± 1 | 78 ± 3 |
| Juglone | Killer | 74% | 85 ± 1 | 61 ± 3 |
| Tannic acid | Killer | 73% | 43 ± 1 | 3 ± 2 |
| 4,4′-diisothiocyanostilbene-2,2′-sufonic acid sodium salt (DIDS) | Killer | 69% | 58 ± 4 | 56 ± 5 |
| Phenylmercuric acetate | Killer | 69% | 50 ± 6 | 59 ± 2 |
| Verteporfin | Prestwick | 69% | 41 ± 5 | 38 ± 5 |
| Clofazimine | Prestwick | 47% | 30 ± 7 | 28 ± 5 |
| NSC 95397 (2,3bis[(2-Hydroxyethyl)thio]-1,4-naphthoquinone) | Tocris | 68% | 58 ± 8 | 58 ± 1 |
| NSC 3852 (5-Nitroso-8-quinolinol) | Tocris | 58% | 48 ± 5 | 47 ± 5 |
| Ro-08-2750 (2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde) | Tocris | 55% | 59 ± 3 | 69 ± 8 |
| Chlorophyllide Cu complex Na salt | US Drugs | 80% | 97 ± 1 | 78 ± 3 |
| Tannic acid | US Drugs | 73% | 43 ± 1 | 3 ± 2 |
| Phenylmercuric acetate | US Drugs | 52% | 29 ± 4 | 32 ± 4 |
| Nitrofurazone | US Drugs | 52% | 54 ± 2 | 48 ± 5 |
| Pyrvinium pamoate | US Drugs | 49% | 468 ± 1 | 36 ± 3 |
| Hexachlorophene | US Drugs | 48% | 12 ± 1 | 1 ± 1 |
| ST012942* | NPL-640 | 86% (15 μM) | 96 ± 1 (15 μM) | 79 ± 2 (15 μM) |
| Dehydroglaucine* | NPL-640 | 62% (17 μM) | 82 ± 4 (17 μM) | 57 ± 8 (17 μM) |
| Gossypolone* | NPL-640 | 57% (12 μM) | 30 ± 5 (12 μM) | 25 ± 4 (12 μM) |