Inhibition of hPGHS-2 and hPGHS-2(R106E) by acidic and nonacidic NSAIDs
| Inhibitor | IC50hPGHS-2 | n | IC50hPGHS-2(R106E) | n | Ratio IC50hPGHS-2(R106E)/hPGHS-2 |
|---|---|---|---|---|---|
| nm | nm | ||||
| NS-398 | 7.2 ± 0.9 | 8 | 7,440 ± 2,000 | 6 | 1,030 |
| Flosulide | 43.9 ± 4.1 | 5 | >30,000 | 5 | >683 |
| Flurbiprofen | 35.9 ± 13.5 | 5 | 34,700 ± 8,680 | 6 | 965 |
| Diclofenac | 3.3 ± 0.6 | 6 | 15 ± 1.7 | 6 | 4.5 |
| Meclofenamic acid | 3 ± 0.3 | 7 | 16.4 ± 2 | 7 | 5.5 |
| Indomethacin | 39.6 ± 5.0 | 11 | 1,899 ± 354 | 13 | 47.9 |
| L-588,983 | 19.7 ± 7.6 | 4 | 6.6 ± 2.9 | 4 | 0.3 |
| L-761,066 | 352 ± 57 | 6 | 7,370 ± 2,730 | 4 | 20.9 |
| L-746,483 | 1.4 ± 0.5 | 5 | 2.8 ± 0.3 | 6 | 2 |
| DuP697 | 1.3 ± 0.2 | 7 | 1.8 ± 0.3 | 7 | 1.4 |
| L-745,296 | 8,300 ± 2,890 | 4 | 1,960 ± 290 | 7 | 0.24 |
IC50 values for various inhibitors were determined in intact CHO cells stably expressing hPGHS-2 and hPGHS-2(R106E) as described in the legend to Fig. 5 and in Materials and Methods. The values represent the average ± standard deviation of four to 13 separate experiments (n).