Chemical Name: 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
Biological ActivityPotent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 values are 4 and 23 nM for TGF-β type I receptor autophosphorylation and binding respectively). Selective for TGF-β type I receptor over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). Enhances the efficiency of cellular reprogramming; replaces Sox2 by inducing Nanog expression.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-γ type I receptor inhibitors.
Gellibert et al.
Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors.
Li et al.
Cell Stem Cell, 2009;4:16
A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog.
Ichida et al.
Cell Stem Cell, 2009;5:491
Citations for RepSox
The citations listed below are publications that use Tocris products. Selected citations for RepSox include:
6 Citations: Showing 1 - 6
Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals.
Authors: Yung Et al.
Single cell analysis of human foetal liver captures the transcriptional profile of hepatobiliary hybrid progenitors.
Authors: Segal Et al.
Nat Commun 2019;10:3350
Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages.
Authors: Lichtenberger Et al.
Nat Commun 2016;7:10537
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
GARP-TGF-β complexes negatively regulate regulatory T cell development and maintenance of peripheral CD4+ T cells in vivo.
Authors: Zhou Et al.
J Immunol 2013;190:5057
Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments.
Authors: Li Et al.
Am J Physiol Renal Physiol 2013;13:1969
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Mice received a dose of 1 μmol RepSox or vehicle only topically onto the back skin.