Table 2. Effect on IL-8 secretion and TAT activity in cell lines.
| IL-8 inhibition IC50, nM | IL-8 inhibition efficacy, % | TAT induction EC50, nM | TAT induction efficacy, % | |
|---|---|---|---|---|
| DEX. | 2.6 ± 1 | 100 | 0.3 | 100 |
| PRED | 18 ± 12 | 92 ± 8 | 1.5 | 100 |
| ZK 216348 | 35 ± 10 | 52 ± 15 | 95 | 88 |
Inhibition of IL-8 secretion in monocytic THP-1 cells as a parameter for transrepression and induction of TAT in hepatic H4-II-E-C3 cells as a transactivation parameter were determined for ZK 216348 in comparison to standard GCs. Efficacy is expressed relative to the maximal response to DEX. For IL-8 inhibition, mean ± SD values of three to five separate experiments are shown, whereas single values are given for TAT induction.