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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
  1. IL-6 values are expressed as mean ± SD. IL-6 release of vehicle-treated cells was set to 100% (n = 2). Seven out of 9 HAK compounds suppressed significantly the OSM-induced IL-6 release. There was no intimate correlation between significant IL-6 reduction (bold) and the potency of HAK compounds to inhibit activity of recombinant prolyl endopeptidase (bold), presented as Ki values. All amino acids were used in L-configuration. Z, benzyloxycarbonyl, BTh, benzothiazole, Th, thiazole.