Figure 6.

Preliminary screening using the novel cell-based assay established above and verification of the active compounds. (A) A total of 474 compounds in the small molecular compound library were screened, and of them, ten compounds (above line) demonstrated some antagonistic activities against membrane IL-6R. Each dot represents one compound. (B) The functional identification of the three active compounds selected using a widely used method based on the soluble receptor-ligand binding assay. Three compounds were able to block soluble IL-6R from binding to its ligand in a dose-dependent manner. The data represent the mean±SEM from five separate experiments. (C and D) The compounds inhibited the proliferation of the 7TD1 cells (or the phosphorylation of STAT3 in the U937 cells) induced by IL-6. The data represent the mean±SEM from four independent experiments. ^cP<0.01, significant compared with the untreated control; ^eP<0.05, ^fP<0.01, significant compared with IL-6 alone.