Table 2.
Summarized effects on TrxR1 by explored STAT3 inhibitors.
| Compound | Inhibition of purified TrxR1 | Inhibition of cellular TrxR1 | Tm with NADPH | Tm without NADPH | Substrate of TrxR1 |
|---|---|---|---|---|---|
| Auranofin | ++++ | ++ | 46.4 °C | 66.6 °C | – |
| Stattic | +++ | +++ | 66.6 °C | 66.4 °C | + |
| S3I-1757 | +++ | – | 50.8 °C | 67.2 °C | – |
| 5,15-DPP | ++ | ++ | 50.6 °C | 67.2 °C | – |
| Galiellalactone | ++ | + | 50.6 °C | 66.6 °C | – |
| LLL12 | ++ | ++ | 69.0 °C | 66.5 °C | + |
| Cpd188 | + | – | 68.0 °C | 67.4 °C | + |
| Napabucasin | + | + | 68.4 °C | 67.2 °C | + |
| BP1-102 | + | + | – | – | – |
| STA-21 | + | + | 52.4 °C | 66.9 °C | – |
| inS3-54 | + | – | 51.8 °C | 66.6 °C | – |
| SH-4-54 | + | – | 51.0 °C | 67.9 °C | – |
| S3I-201 | + | + | 51.2 °C | 67.3 °C | – |
| STX-0119 | (+) | – | 51.4 °C | 67.1 °C | – |
| Degrasyn (WP1130) | ++ | ++ | 52.5 °C | 66.5 °C | – |
| WP1066 | + | – | 52.4 °C | 65.7 °C | – |
| Cucurbitacin I (JSI-124) | (+) | – | 52.8 °C | 66.9 °C | – |
| Tyrphostin B42 (AG490) | (+) | – | 51.5 °C | 66.8 °C | – |
| Cryptotanshinone | ++ | – | 62.9 °C | 66.9 °C | + |
| Disulfiram | + | – | 58.3 °C | 58.8 °C | + |
| Pyrimethamine | – | – | 50.9 °C | 66.5 °C | – |
| Celecoxib | – | – | 51.2 °C | 66.7 °C | – |
| Atovaquone | – | – | 50.4 °C | 66.8 °C | – |
Underlining is indicative of a signficant change in Tm compared to DMSO-treated TrxR1.