SM 16

Biological Activity

SM 16 is a potent TGF-β receptor type 1 (TGF-βRI) inhibitor (IC₅₀ = 64 nM in luciferase assay). Selective for TGF-βRI over other ALK family members. Decreases Smad phosphorylation and inhibits tumor growth in a mouse xenograft model. Attenuates increased TGF-β signaling in retinal vessels of diabetic rats. Also prevents intimal thickening and vascular remodeling in rat carotid balloon injury model. Orally bioavailable.

Technical Data

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.

Background References

1. The increased transforming growth factor-β signaling induced by diabetes protects retinal vessels.
   Dagher et al.
   Am.J.Pathol., 2017;187:627
2. A novel small-molecule inhibitor of transforming growth factor β type I receptor kinase (SM16) inhibits murine mesothelioma tumor growth in vivo and prevents tumor recurrence after surgical resection.
   Suzuki et al.
   Cancer Res., 2007;67:2351
3. SM16, an orally active TGF-β type I receptor inhibitor prevents myofibroblast induction and vascular fibrosis in the rat carotid injury model.
   Fu et al.
   Arterioscler.Thromb.Vasc.Biol., 2008;28:665

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