Table 5.
Confirmation of the Library of Pharmacologically Active Compounds and National Institutes of Health Clinical Collection Primary pSTAT3 High-Content Screening Actives
| Compound information | % Inhibition of IL-6-induced pSTAT3-Y705 | % Inhibition of IFNγ–induced pSTAT1-Y701 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| SID | SL | Name | HCS | Mean 24 h | SD | Mean 1 h | SD | Mean 24 h | SD | Mean 1 h | SD |
| 46386661 | N | Azelastine | 82.6 | 90.4 | 4.8 | 96.2 | 14.5 | 24.2 | 18.1 | 29.6 | 41.4 |
| 53777461 | L | Dihydroouabain | 97.8 | 84.2 | 6.2 | 4.7 | 16.9 | 81.3 | 8.0 | −55.5 | 19.0 |
| 53777973 | L | NF449 octasodium salt | 85.2 | 72.6 | 5.2 | 96.9 | 2.7 | 90.3 | 7.8 | 96.1 | 1.4 |
| 46386563 | N | Desloratadine | 72.9 | 72.0 | 1.5 | 111.3 | 1.0 | 27.4 | 22.2 | 73.5 | 8.5 |
| 53778225 | L | SB 205384 | 85.0 | 69.8 | 7.0 | 56.6 | 2.8 | 89.2 | 1.4 | 25.4 | 1.1 |
| 53778026 | L | Phenylephrine hydrochloride | 51.6 | 69.5 | 4.7 | 85.4 | 1.3 | 40.2 | 4.6 | 75.9 | 5.3 |
| 53778265 | L | Trazodone hydrochloride | 53.5 | 68.2 | 4.5 | 72.0 | 3.9 | 35.7 | 12.4 | 50.5 | 15.2 |
| 46387007 | N | R(+)-SCH-23390 HCl | 63.4 | 66.4 | 5.5 | 77.1 | 2.5 | 30.5 | 23.8 | 65.6 | 3.1 |
| 53778017 | L | Nylidrin hydrochloride | 59.8 | 66.1 | 8.7 | 72.4 | 3.6 | 20.7 | 12.0 | 45.7 | 16.9 |
| 53778204 | L | Albuterol hemisulfate | 60.2 | 63.5 | 2.3 | 102.8 | 2.1 | 20.9 | 9.0 | 94.0 | 1.7 |
| 53777777 | L | Isotharine mesylate | 52.1 | 59.1 | 9.5 | 23.0 | 2.3 | −11.0 | 5.5 | −29.6 | 13.2 |
| 53777593 | L | Forskolin | 75.2 | 57.2 | 4.8 | 91.3 | 1.8 | 3.8 | 9.6 | 84.4 | 3.5 |
| 46386983 | N | Etomidate | 61.3 | 56.7 | 7.1 | 65.8 | 8.1 | 17.1 | 22.3 | 13.4 | 7.8 |
| 53777746 | L | R(−)-Isoproterenol (+)-bitartrate | 64.4 | 56.1 | 1.8 | 52.8 | 4.8 | 27.0 | 5.2 | 44.6 | 12.2 |
| 53777650 | L | Fenoterol hydrobromide | 61.5 | 56.0 | 10.0 | 107.5 | 1.7 | 7.5 | 16.2 | 97.0 | 1.2 |
| 46386731 | N | Cefpodoxime proxetil | 55.1 | 54.6 | 1.1 | 99.0 | 3.3 | 13.1 | 18.6 | 94.0 | 2.7 |
| 53778255 | L | Tulobuterol hydrochloride | 57.5 | 53.0 | 11.4 | 60.6 | 5.6 | 22.6 | 8.2 | 57.5 | 7.7 |
| 53778281 | L | Tyrphostin AG 879 | 59.1 | 52.4 | 6.9 | 27.8 | 10.6 | 53.5 | 10.6 | 52.4 | 20.6 |
| 53777778 | L | (−)-Isoproterenol hydrochloride | 69.4 | 52.2 | 9.3 | 66.2 | 7.2 | 25.2 | 22.2 | 52.2 | 16.6 |
| 53777840 | L | Metaproterenol hemisulfate | 58.5 | 51.3 | 0.7 | 102.6 | 3.0 | 8.1 | 26.1 | 93.1 | 0.7 |
| 53777465 | L | (−)-α-methylnorepinephrine | 55.8 | 51.2 | 9.1 | 68.1 | 3.3 | 27.4 | 16.0 | 12.7 | 6.2 |
| 53778191 | L | (±)-Synephrine | 61.5 | 50.7 | 7.8 | 59.6 | 7.4 | 12.3 | 22.3 | 50.8 | 16.3 |
| 53777817 | L | (±)-Isoproterenol hydrochloride | 63.4 | 50.3 | 2.6 | 63.9 | 3.3 | 17.8 | 20.7 | 32.1 | 33.1 |
| 53778152 | L | Cortexolone maleate | 57.1 | 50.3 | 6.2 | 46.5 | 3.5 | 5.6 | 21.3 | −35.5 | 30.4 |
| 53777595 | L | N-(3,3-diphenylpropyl)glycinamide | 61.0 | 49.6 | 11.6 | 62.6 | 2.7 | 9.3 | 15.4 | 34.3 | 5.8 |
| 53778147 | L | Ritodrine hydrochloride | 63.1 | 49.0 | 2.6 | 69.7 | 12.7 | −3.1 | 17.6 | 48.0 | 7.9 |
| 53778120 | L | Propantheline bromide | 57.0 | 47.7 | 9.9 | 53.4 | 3.0 | 11.7 | 26.7 | 35.6 | 8.2 |
| 46386828 | N | Balsalazida | 58.5 | 47.1 | 3.0 | 53.1 | 4.0 | 10.0 | 29.3 | 15.4 | 25.4 |
| 53778232 | L | Terbutaline hemisulfate | 61.4 | 46.3 | 6.1 | 97.6 | 2.6 | −12.4 | 16.9 | 78.4 | 8.3 |
| 53778036 | L | Perphenazine | 73.3 | 46.2 | 2.8 | 87.3 | 7.7 | 50.9 | 8.5 | 68.5 | 0.7 |
| 53777521 | L | 6,7-ADTN hydrobromide | 52.8 | 45.7 | 6.3 | 50.4 | 9.4 | 19.1 | 19.6 | 32.8 | 3.6 |
| 53777200 | L | L(−)-Norepinephrine bitartrate | 55.8 | 40.5 | 10.9 | 61.9 | 2.2 | 34.3 | 23.7 | 39.1 | 10.9 |
| 46387005 | N | Salmeterol | 63.2 | 38.5 | 4.8 | 110.4 | 1.4 | 2.8 | 26.3 | 90.0 | 1.9 |
| 53777665 | L | Guanidinyl-naltrindole di-trifluoroacetate | 57.8 | 36.8 | 12.2 | 52.7 | 5.2 | −13.6 | 10.0 | −15.3 | 7.6 |
| 53777160 | L | Aurintricarboxylic acid | 86.3 | 36.5 | 5.4 | 105.0 | 0.8 | 99.4 | 0.2 | 98.6 | 2.5 |
| 53777487 | L | 8-Cyclopentyl-1,3-dipropylxanthine | 52.1 | 33.8 | 10.6 | 60.6 | 4.6 | 23.8 | 15.0 | 26.6 | 18.3 |
| 53777634 | L | cis-(Z)-flupenthixol dihydrochloride | 79.0 | 30.8 | 10.1 | 72.3 | 5.3 | 13.3 | 13.2 | 15.5 | 23.4 |
| 53777608 | L | (−)-Epinephrine bitartrate | 62.1 | 24.7 | 11.4 | 58.0 | 7.4 | 1.6 | 16.5 | 11.1 | 15.7 |
| 53777159 | L | (±)-Norepinephrine (+)bitartrate | 69.5 | 24.4 | 7.6 | 62.1 | 2.2 | 43.4 | 12.2 | 45.6 | 11.0 |
HCS data represent % inhibition of a single well, confirmation data represent mean % inhibition±SD (n=3), 1 and 24 h of compound exposure data presented.
SID, PubChem substance identifier, SL, source library, L, LOPAC, N, NIH CC.