tgfβri in 3

TGFβRI-IN-3 is a highly selective TGFβR1 inhibitor with an IC50 of 0.79 nM and exhibits 2000-fold selectivity against MAP4K4, showing potential applications in immuno-oncology [1].

TGFβRI-IN-7 (compound 16W) is a potent inhibitor of TGFβRI. It effectively inhibits the phosphorylation of SMAD2/3 and reduces the viability of H22 cells, with IC50 values of 12 nM and 65 nM, respectively. In an H22 cell xenograft model, TGFβRI-IN-7 exhibits antitumor efficacy with a TGI of 79.6%.

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.