RepSox (446859-33-2) is a potent (IC50 ALK5 auto-P= 4 nM; IC50 TGF-β cellular assay = 23 nM) inhibitor of the TGF-β type I receptor (ALK5).1 RepSox can replace Sox2 in reprogramming adult cells into pluripotent stem cells via induction of Nanog transcription.2 It was able to convert astrocytes into neuronal cells as part of a small molecule cocktail (along with valproic acid and CHIR99021).3,4
References/Citations:
1) Gellibert et al. (2004), Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-β Type I Receptor Inhibitors; J. Med. Chem. 47 4494
2) Ichida et al. (2009), A Small-molecule Inhibitor of TGF-β Signaling Replaces Sox2 in Reprogramming by Inducing Nanog; Cell Stem Cell 5 491
3) Cheng et al. (2015), Direct Conversion of astrocytes into neuronal cells by a drug cocktail; Cell Res. 25 1269
4) Cheng et al. (2014), Generation of neural progenitor cells by chemical cocktails and hypoxia; Cell Res. 24 665
