Table 2.
Inhibition of NR-mediated transcription in the presence of compound PS121912 using luciferase-based transcription assays in HEK293T cells activated by different NR agonists.
| Compound | Nuclear Receptor | IC50 (μM)8 |
|---|---|---|
| 1 | VDR | 0.59 ± 0.11 |
| 2 | PPAR-α | 20.8 ± 1.12 |
| 3 | PPAR-γ | >253 |
| 4 | PPAR-δ | >304 |
| 5 | RxR-α | >255 |
| 6 | TR-α | >306 |
| 7 | TR-β | 24.1 ± 1.16 |
| 8 | ER-α | 26.2 ± 3.37 |
| 9 | ER-β | >257 |
1
1,25(OH)2D3(10nM),
2
GW7647 (30nM),
3
Rosiglitazone (300nM),
4
GW0742 (50nM),
5
Bexarotene (200nM),
6
T3 (10nM),
7
estradiol (10nM),
8
three independent experiments were conducted in quadruplicate and data was analyzed using nonlinear regression with variable slope (GraphPrism).