TGFβRII-IN-3

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) (IC₅₀ = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research^[1].

TGFβRII-IN-3 (5-15 μM; 24 h) inhibits the activity of the TGFβ signaling pathway by reducing the phosphorylation level of Smad2 in A549 cells. It also selectively degrades TGFβ RII ^[1].
TGFβRII-IN-3 (2.5-10 μM; 48 h) effectively inhibits TGFβ1-induced E-cadherin loss in A549 cells, while simultaneously suppressing the upregulation of Snail and N-cadherin ^[1].
TGFβRII-IN-3 (5 μM; 48 h) inhibits cell migration and morphological changes in A549 and H1299 cells by inhibiting TGFβ signaling ^[1].

References:
[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.

TGFβRII-IN-3 (Compound 2r) 是一种选择性的 TGFβ 类型 II 受体 (TGFβ RII) 的抑制剂 (IC₅₀= 4.1 μM)。其通过促进 TGFβ RII 的蛋白质降解来抑制 TGFβ 信号传导。TGFβRI-IN-7 可以阻断内皮向间充质的转变和细胞迁移。TGFβRI-IN-7 还能够用于癌症研究。

TGFβRII-IN-3 (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。
TGFβRII-IN-3 (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。
TGFβRII-IN-3 (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。