| Bioactivity | STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibits STAT3 phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced by TGF-β1 and inhibit epithelial-mesenchymal transition (EMT)[1]. |
| Invitro | STAT3-IN-15 (化合物 10k) 抑制 NIH-3T3 细胞增殖，IC50 为 0.47 μM[1]。STAT3-IN-15 与 Lys591 和 Ser636 形成氢键，占据 STAT3 的 pY 子袋。[1]。STAT3-IN-15 (0-100 nM, 72 h) 抑制成纤维细胞活化和增殖[1]。STAT3-IN-15 (50 nM, 24 h) 抑制 TGF-β1 (5 ng/mL) 诱导的 NIH-3T3 细胞激活[1]。STAT3-IN-15 (200 nM，24 小时) 阻断 A549 细胞中 TGF-β1 诱导的 EMT 过程 (形态学变化)[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | STAT3-IN-15 (化合物 10k) (30 和 60 mg/kg，灌胃给药) 减轻 Bleomycin (HY-108345) 诱导的小鼠肺纤维化[1]。 Animal Model: |
| Name | STAT3-IN-15 |
| Formula | C20H17F3N2O3S |
| Molar Mass | 422.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang Y, et al. Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis. Eur J Med Chem. 2022 Nov 28;246:114953. |