| Bioactivity | TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research[1]. |
| Invitro | TGFβ1-IN-3 (compound 44) 对 NIH-3T3 细胞具有抑制作用，IC50 为 0.57 μM[1]。TGFβ1-IN-3 (compound 44; 10 μM; for 24 h) 抑制 TGF-β1 诱导的 NIH-3T3 和 A549 细胞的异常激活，以及 A549 细胞的迁移和上皮-间质转化 (EMT) [1].TGFβ1-IN-3 (compound 44) 可与 STAT3 结合，并可与 Ile659 相互作用，亲水基团哌啶与 Ser636、Arg609、Pro639 形成分子间作用力。TGFβ1-IN-3 的硝基呋喃可与 Lys658 相互作用[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | TGFβ1-IN-3 (compound 44; 30-60 mg/kg; p.o; once daily; for 22 days) 改善小鼠肺功能并减缓 IPF 的进展。TGFβ1-IN-2可逆转治疗模型中的肺纤维化[1]。 Animal Model: |
| Name | TGFβ1-IN-3 |
| Formula | C23H30N4O5 |
| Molar Mass | 442.51 |
| 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]. Xingping Su, et al. Design, synthesis and biological evaluation of novel diarylacylhydrazones derivatives for the efficient treatment of idiopathic pulmonary fibrosis. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114918. |