Table 2. Summary of activity of compounds in inhibiting Stat3 binding to pY peptide ligand in a surface plasmon resonance binding (SPR) assay, in inhibiting IL-6-mediated Stat3 phosphorylation (pStat3) and in inhibiting IL-6-mediated Stat3 nuclear translocation in a high-throughput fluorescence microscopy (HTFM) assay.
Assay | Cpd3 | Cpd30 | Cpd188 | Cpd3-2 | Cpd3-7 | Cpd30-12 |
SPR | 4471 | 30 | 20 | 256 | 137 | 114 |
pStat3 | 91 | 18 | 73 | 144 | 63 | 60 |
HTFM | 131 | 77 | 39 | 150 | 20 | >300 |
Data presented are IC50 values (µM) obtained using results summarized in Figures 1 (SPR), Figure 2 (pStat3) and Figure 4 (HTFM).