Table 1 Effects of HAK compounds on PREP inhibition and on OSM-stimulated IL-6 secretion from U343 cells
From: Heteroarylketones inhibit astroglial interleukin-6 expression via a STAT3/NF-κB signaling pathway
Compound | Z-P2-P1-P1' | Remaining IL-6 expression [% of control] | PREP assay (Ki [M] |
|---|---|---|---|
HAK-1 | Z-Phe-Pro-BTh | 15.9 ± 1.87 | 4.6 × 10 -9 |
HAK-2 | Z-Ala-Pro-BTh | 18.7 ± 3.87 | 3.8 × 10 -11 |
HAK-3 | Z-Phe-Leu-BTh | 22.1 ±5.91 | > 1.0 × 10-6 |
HAK-4 | Z-Phe-Ala-BTh | 35.1 ± 6.75 | > 1.0 × 10-5 |
HAK-5 | Z-Phe-Pro-Th | 35.2 ± 12.92 | 1.1 × 10 -10 |
HAK-6 | Z-Lys-Pro-BTh | 38.8 ± 5.26 | 4.1 × 10 -9 |
HAK-7 | Z-Asp-Pro-BTh | 52.8 ± 3.91 | 1.2 × 10 -8 |
HAK-8 | Z-Arg-Pro-BTh | 96.8 ± 10.69 | 3.2 × 10 -9 |
HAK-9 | Z-Phe-Phe-BTh | 182.8 ± 25.41 | > 1.0 × 10 -5 |