| Bioactivity | RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes[1][2]. | ||||||||||||
| Invitro | RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC50 value of 4 nM[1].RepSox (0-10 μM; 0-8 days) induces adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium[2]. RepSox (0-10 μM; 0-8 days) promotes the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells[2]. RepSox(0-10 μM; 0-8 days) induces brown adipogenesis in primary mouse fibroblasts and fat precursor cells[2]. Western Blot Analysis[2] Cell Line: | ||||||||||||
| Name | RepSox | ||||||||||||
| CAS | 446859-33-2 | ||||||||||||
| Formula | C17H13N5 | ||||||||||||
| Molar Mass | 287.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Gellibert F, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004 Aug 26;47(18):4494-506. [2]. Wan-Zhi Tu, et al. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacol Sin. 2019 Dec;40(12):1523-1531. |