FIGURE 4.
GLEPP1 inhibitors block cellular chemotaxis. Compound 1 and Compound 2 were tested in cellular assays for MCP-1-directed chemotaxis of primary human monocytes (A), the monocytic human THP1 cell line (B and C), and BMDM cells (E). D, correlation between the IC50 values for GLEPP1 inhibitors in vitro (horizontal) with activity in the THP1 cell assay (vertical). Two of the tested compounds failed to show activity in the cell assay at the highest dose tested (50 μm; indicated by arrows). F, Glepp1 mRNA expression analysis (qPCR) following a 2-h exposure of THP-1 cells to 20 μm Compound 1 or 2 or to diluted solvent (DMSO; all biological triplicates).