Potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5), IC50 = 14.3 nM and ALK4 (IC50 = 58.5 nM) with no activity at ALK2, 3 and 61. Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model. It causes...
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Potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5), IC50 = 14.3 nM and ALK4 (IC50 = 58.5 nM) with no activity at ALK2, 3 and 61. Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model. It causes significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis. Sensitizes drug-resistant pancreatic cancer cells to gemcitabine. Cell permeable and active in vivo
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