Cellular activity and enzymatic specificity of RWJ 67657 and SB 203580
| Compound | IC50 | Inhibition | |||||
|---|---|---|---|---|---|---|---|
| LPS/PBMC | |||||||
| TNF-α Release | IL-1β Release | p56 lck 5 μM | c-src 5 μM | PKA 5 μM | ERK-2 10 μM | COX-1 IC50 | |
| nM | % | μM | |||||
| RWJ 67657 | 3 ± 1 | 11 ± 2 | 10 ± 7 | 15 ± 5 | 0 | 11 ± 4 | >10 |
| SB 203580 | 30 ± 12 | 94 ± 19 | 55 ± 8 | 55 ± 18 | 0 | 22 ± 7 | 3.9 ± 2.2 |
Compounds were serially diluted, from an initial concentration of 10 mM, for IC50 determinations, maintaining a constant vehicle (DMSO) concentration (0.1%) in the final assay volume. An IC50value was termed >10 μM if there was a reproducible dose-response but inhibition did not reach 50% at 10 μM. Chemical solubility problems prevented assay of concentrations beyond 10 to 20 μM of RWJ 67657.
Values represent means of 2 to 10 experiments ±1 S.D.