tgfβri-in-1

TGFβRI-IN-1 is an oral active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase(IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively ).

TGFβRI-IN-5 (Compound 4b) 是 TGFβRI 的有效抑制剂，IC50值为 0.08 μM。TGFβRI-IN-5 对所有测试细胞系的均显示出显著的抗癌活性，可增强细胞凋亡并抑制细胞周期的 G2 M 期。

ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1].

TGFβRI-IN-3 抑制TGFβR1，IC50为 0.79 nM，是对 MAP4K4 的选择性2000 倍。TGFβRI-IN-3 是一种高选择性的 TGFβR1 抑制剂，在免疫肿瘤中具有潜在的应用。