Table 7.
EMSA and FP inhibition data of selected inhibitors for disruption of the Stat3–Stat3:DNA and Stat3–gp130 sequence complexes in vitro.
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---|---|---|---|---|---|
Compd | R1 | X | R2 | EMSA IC50 [µm] | FP Ki [µm] |
8 (S3I-201) | H | O | ![]() |
86 ± 33 | > 50 |
27 h | ![]() |
NCH3 | ![]() |
35 ± 9 | 15 ± 4.9 |
27 kd | ![]() |
NCH3 | ![]() |
45 ± 12 | 18.7 ± 1.4 |
27 kd | ![]() |
NCH3 | ![]() |
50 ± 15 | 21.5 ± 2.2 |
27 kd | ![]() |
NCH3 | ![]() |
74.3 ± 9.3 | 21.6 ± 0.9 |
27 kd | ![]() |
NCH3 | ![]() |
43 ± 1.3 | 16.7 ± 1.7 |