Potent and selective inhibitor of TGF-β type I receptor (ALK5). Inhibits Smad-2 phosphorylation (IC50
= 5.3 nM). Exhibits selectivity over a panel of 27 serine/ threonine and tyrosine kinases including P38α. Attenuates TGFβ/Smad signaling, cell migration, invasion, lung metastasis and increases survival of mice in 4TI in vivo
models. Suppresses renal fibrosis in obstructive nephropathy in vivo
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Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/activin receptor-like kinase-5, on prostate cancer cells.
Lee et al.
An novel inhibitor of TGF-� type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition.
Park et al.
Cancer Lett., 2014;351:72
IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy.
Moon et al.
Kidney Int., 2006;70:1234