STAT3-IN-15 是一种有效的，具有口服活性的 STAT3 抑制剂，可对抗特发性肺纤维化 (IPF)。STAT3-IN-15 抑制 STAT3 磷酸化。STAT3-IN-15 还抑制 TGF-β1 诱导的上皮细胞迁移和变形，抑制上皮间质转化 (EMT)。
| 生物活性 | STAT3-IN-15 is a potent and orally activeSTAT3inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibitsSTAT3phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced byTGF-β1and inhibit epithelial-mesenchymal transition (EMT)[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 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: | NIH-3T3 cells | | Concentration: | 0, 6.25, 12.5, 25, 50, 100 nM | | Incubation Time: | 72 h | | Result: | Inhibited NIH-3T3 cell viability dose-dependently. |
Western Blot Analysis[1] | Cell Line: | NIH-3T3 cells | | Concentration: | Inhibited NIH-3T3 cell viability dose-dependently. | | Incubation Time: | 24 h | | Result: | Inhibited the expression of α-SMA and collagen I and the phosphorylation of STAT3. |
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体内研究
(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: | BLM-induced pulmonary fibrosis mouse model[1] | | Dosage: | 30 and 60 mg/kg | | Administration: | Intragastric administration | | Result: | Recovered the lung structure and reduced the hydroxyproline content.
Reduced the expression of the p-Stat3Ty705protein in the lung tissue.
Improved BLM-induced imbalance of immune microenvironment. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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