W1131

W1131 is a STAT3 inhibitor. It selectively inhibits the phosphorylation of STAT3 over STAT1, STAT5, JAK2, and Akt in AGS gastric adenocarcinoma cells at 3 µM. W1131 binds to STAT3 in a cell-free assay (Kd = 7. µM) and increases the thermal stability of STAT3 in a cellular thermal shift assay (CETSA) using AGS cells when used at a concentration of 1 µM. It also inhibits STAT3 dimerization, nuclear accumulation, and transcriptional activation in cell-based assays. W1131 (3 µM) induces cell death in AGS cells, which can be reversed by Z-VAD-FMK (Z-VA-DL-D(OMe)-FMK, Cay-27421), ferrostatin-1 (Cay-17729), liproxstatin-1 (Cay-17730), deferoxamine (DFO, Cay-14595), necrosulfonamide (Cay-20844), or bafilomycin A1 (Cay-11038). In vivo, W1131 (10 mg/kg) decreases tumor volume and weight in 5-fluorouracil-sensitive and -resistant MGC803 gastric cancer mouse xenograft models.. Solulibility: DMSO: Slightly soluble: 0.1-1 mg/ml: .