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.

1117684-36-2

C18H18N4O3S

370.43

AZ 12799734

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years