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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 420.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.38 mL||11.89 mL||23.78 mL|
|5 mM||0.48 mL||2.38 mL||4.76 mL|
|10 mM||0.24 mL||1.19 mL||2.38 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the products' biological activity.
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/activin receptor-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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