- Potent inhibitor of transforming growth factor-β type I receptor (TGF-βRI; ALK5) (IC50 = 17 nM in cellular inhibition assay and 47 nM in TGF-β-induced luciferase activity assay).
- Also inhibits ALK4, ALK6 and ALK7 at concentrations under 10 μM.
- Inhibits BMP signaling, phosphorylation of SMAD1 and SMAD2, and TGF-β-induced epithelial cell migration in vitro.
- Displays cardiotoxicity in vivo.
- Orally bioavailable.
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