| Identification | Back Directory | [Name]
1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-, hydrochloride (1:1) | [CAS]
2319939-07-4 | [Synonyms]
1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-, hydrochloride (1:1) | [Molecular Formula]
C17H14ClN5 | [MOL File]
2319939-07-4.mol | [Molecular Weight]
323.78 |
| Hazard Information | Back Directory | [Description]
ALK5 inhibitor II is a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively).1 This inhibitor demonstrated less potent activity (IC50s > 16 μM) when tested against a panel of 9 related kinases, including p38 MAPK and GSK3.1 At 25 μM, this compound has been used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2 via inhibition of the TGF-β signaling pathway and induction of Nanog transcription.2 This product is a hydrochloride form of the compound. A non-hydrochloride version of ALK5 inhibitor II is also available. | [Uses]
RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes. | [References]
1. Gellibert, F., Wollven, J., Fouchet, M.H., et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-β type I receptor inhibitors J. Med. Chem. 47(18),4494-4506(2004).
2. Ichida, J.K., Blanchard, J., Lam, K., et al. A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog Cell Stem Cell 5(5),491-503(2009). |
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