TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) with an IC50 of 4.1 μM. It inhibits TGFβ signaling by promoting protein degradation of TGFβ RII. Additionally, TGFβRI-IN-7 can block the transition from endothelial to mesenchymal states and inhibit cell migration, making it useful for cancer research.

TGFβRII:4.1 μM

TGFβRII-IN-3 effectively inhibits the activity of the TGFβ signaling pathway in A549 cells by reducing the phosphorylation levels of Smad2 at concentrations of 5-15μM over 24 hours and selectively degrades TGFβ RII. At concentrations of 2.5-10μM over 48 hours, it also prevents TGFβ1-induced loss of E-cadherin and suppresses the upregulation of Snail and N-cadherin in A549 cells. Furthermore, TGFβRII-IN-3 at 5μM over 48 hours hampers the migration and morphological changes of A549 and H1299 cells by inhibiting TGFβ signal transduction.