Description
RepSox (446859-33-2) is a potent (IC50ALK5 auto-P= 4 nM; IC50TGF-β cellular assay = 23 nM) inhibitor of the TGF-β type I receptor (ALK5).1RepSox can replace Sox2 in reprogramming adult cells into pluripotent stem cells via induction of Nanog transcription.2It was able to convert astrocytes into neuronal cells as part of a small molecule cocktail (along with valproic acid and CHIR99021).3,4
Uses
Alk 5 Inhibitor II is a selective ATP competitive inhibitor of transforming growth factor-β (TGFβ). A potential drug for the treatment of fibrosis and cancer.
Uses
RepSox has been used as an inhibitor of autophosphorylation of the transforming growth factor β type I receptor kinase (ALK5). It has also been used as a basal media component for culturing human Pluripotent stem cells.
Definition
ChEBI: 1,5-naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1h-pyrazol-4-yl]- is a pyrazolopyridine.
Biochem/physiol Actions
RepSox Inhibits TGF-beta receptor signaling. Retroviral transduction of Sox2, Oct4, and Klf4 genes results in direct reprogramming of somatic cells into induced pluripotent stem cells (iPSCs).
References
[1] FRANÇOISE GELLIBERT. Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors[J]. Journal of Medicinal Chemistry, 2004, 47 18: 4494-4506. DOI:
10.1021/jm0400247[2] JUSTIN K ICHIDA. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog.[J]. Cell stem cell, 2009, 5 5: 491-503. DOI:
10.1016/j.stem.2009.09.012[3] LIN CHENG. Direct conversion of astrocytes into neuronal cells by drug cocktail[J]. Cell Research, 2015, 25 11: 1269-1272. DOI:
10.1038/cr.2015.120[4] LIN CHENG. Generation of neural progenitor cells by chemical cocktails and hypoxia[J]. Cell Research, 2014, 24 6: 665-679. DOI:
10.1038/cr.2014.32
