| Solution Information | help | |
| Enzyme: | Signal transducer and activator of transcription 3 [702-738,740-752] | |
| inhibitor: | BDBM43697 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this assay is to determine whether powder samples of compounds identified as possible STAT1 activator probes are nonselective due to activation of STAT3. In this assay activation of STAT3 transcription was measured using a human U3A fibrosarcoma cell line that stably expresses a human STAT3-luciferase construct. This cell line is deficient in STAT1. Test compounds were screened for their ability to increase IL-6-mediated STAT3::luciferase reporter activity. Cells were exposed to test compounds, followed by treatment with IL-6 to activate STAT3 transcription. Changes in STAT3::luciferase activity were monitored by measuring well luminescence. An activator will increase IL-6-mediated STAT3 transcription, thus enhancing the activity of the luciferase reporter gene, and increasing well luminescence. As designed, test compounds that increase STAT3 activity are considered non-selective activators. Compounds were tested in triplicate using a 10-point, 1:3 dilu | |
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