Chemical Name: 4-[[4-[(2.6-Dimethyl-3-pyridinyl)oxy]-2-pyridinyl]amino]benzenesulfonamide
Biological ActivityPotent 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Preclinical evaluation of AZ12601011 and AZ12799734, inhibitors of transforming growth factor β superfamily type 1 receptors.
Spender et al.
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Goldberg et al.
Induction of heart valve lesions by small-molecule ALK5 inhibitors.
Anderton et al.
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