IN 1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂，对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。
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 models.
Moon et al (2006) IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 70 1234 PMID:16929250 |Lee et al (2008) Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/AVNreceptor-like kinase-5, on prostate cancer cells. J.Urol. 180 2660 PMID:18951571 |Park et al (2014) An novel inhibitor of TGF-beta type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 351 72 PMID:24887560
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