Biological Activity
R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
In Vitro
R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor β (TGF-β) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 μM).[1]
In Vivo
Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.