| Bioactivity | TGFβRI-IN-7 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRI-IN-7 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRI-IN-7 can block endothelial-to-mesenchymal transition and cell migration. TGFβRI-IN-7 can be used in cancer research[1]. |
| Invitro | TGFβRI-IN-7 (5-15μM; 24 h) 通过降低 A549 细胞中的 Smad2 的磷酸化水平来抑制 TGFβ 信号通路的活性。并且对 TGFβ RII 的选择性降解作用[1]。TGFβRI-IN-7 (2.5-10 μM; 48 h) 能有效抑制 A549 细胞中的由 TGFβ1 诱导的 E-cadherin 丢失，同时抑制 Snail 和 N-cadherin 的上调[1]。TGFβRI-IN-7 (5 μM; 48h) 通过抑制 A549 和 H1299 细胞对 TGFβ 信号传导，从而抑制了细胞迁移和形态变化[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> TGFβRI-IN-7 相关抗体: Western Blot Analysis[1] Cell Line: |
| Formula | C26H25F3N2O2 |
| Molar Mass | 454.48 |
| 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]. Längle D, et al.Expanding the Chemical Space of Transforming Growth Factor-β (TGFβ) Receptor Type II Degraders with 3,4-Disubstituted Indole Derivatives. ACS Pharmacol Transl Sci. 2024 Mar 21;7(4):1069-1085. |