TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.In Vitro: TGFβ1-IN-1 (compound 42) (0-20 μM, 72 h) inhibits the proliferation of TGF-β1 (5 ng/mL)-treated LX- 2 cells and inhibits LO2 cell viability with an IC 50 of 105 μM.
In Vivo: TGFβ1-IN-1 (compound 42) (p.o., 15 or 30 mg/kg, daily, 3weeks) prevents CCl4-induced liver injury and fibrosis, inhibits the activation of hepatic stellate cell (HSC) and epithelial-mesenchymal transition (EMT), and improves the immune microenvironment of CCl4-induced liver fibrosis as well as CCl4-induced systemic toxicity in C57BL/6J mice.