Table 1.
IC50 values of 7g and 8a-f,j-l against CARM1, PRMT1, and SET7.
| compd | IC50 (μM)
|
||
|---|---|---|---|
| CARM1/PABP1 | PRMT1/NPL3 | SET7/H3 | |
| 7g | 8.6 ± 0.8 | > 667 | > 667 |
| 8a | 10.3 ± 3.3 | > 667 | > 667 |
| 8b | 15.2 ± 0.9 | > 667 | > 667 |
| 8c | 11.9 ± 2.3 | > 667 | > 333 |
| 8d | 12.5 ± 6.1 | > 667 | > 667 |
| 8e | 8.1 ± 2.2 | > 667 | 174 ± 28 |
| 8f | 12.2 ± 3.0 | > 667 | > 600 |
| 8j | 14.8 ± 2.5 | > 667 | > 667 |
| 8k | 16.0 ± 3.8 | > 667 | > 667 |
| 8l | 14.4 ± 1.7 | > 667 | 149 ± 26 |
a
Values were determined from at least two separate experiments. The reaction contained 0.1 μM of GST-CARM1 and 0.5 μM of GST-PABP1, 0.15 μM of GST-PRMT1 and 0.5 μM GST-NPL3, or 0.15 μM of GST-SET7 and 1.1 μM of histone H3 with 0.22 μM [3H] AdoMet and different concentrations of each compound for IC50 determinations with different concentrations of each compound for IC50 determinations. The software that we used for fitting curves and determining IC50s is SigmPlot. The equation used for fitting is y=y0 + a/1+(x/x0)b.