Chemical Name: 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]bicyclo[2.2.2]octane-1-carboxamide
Biological ActivityPotent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The increased transforming growth factor-β signaling induced by diabetes protects retinal vessels.
Dagher et al.
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
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.
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