IN-1130 is a highly selective inhibitor of transforming growth factor-β type I receptor kinase (ALK5) (IC50: 5.3 nM for ALK5-mediated Smad3 phosphorylation). IN-1130 inhibits ALK5 phosphorylation of casein (IC50: 36 nM) and p38α mitogen-activated protein kinase (IC50: 4.3 μM).

IN-1130 (0.5, 1 μM; for 2 hours) suppresses TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells. IN-1130 (1 μM; pretreated for 30 min) suppresses TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion. IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) suppresses TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells [2].

IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys. IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) decreases the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats[1]. IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].

868612-83-3

C25H20N6O

420.47

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years