RepSox

Cat. No. 3742

RepSox C17H13N5 [446859-33-2]

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Alternative Names: E-616452, SJN 2511, ALK5 Inhibitor II

Chemical Name: 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine

Biological Activity

Potent 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.

Technical Data

M.Wt:
287.32
Formula:
C17H13N5
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
446859-33-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Ichida et al (2009) A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 5 491. PMID: 19818703.

Li et al (2009) Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 4 16. PMID: 19097958.

Gellibert et al (2004) Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-γ type I receptor inhibitors. J.Med.Chem. 47 4494. PMID: 15317461.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for RepSox include:

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217. PMID: 27320041.

Li et al (2013) Flow-based pipeline for systematic modulation and analysis of 3D tumor microenvironments. Am J Physiol Renal Physiol 13 1969. PMID: 23563587.

Zhou et al (2013) GARP-TGF-β complexes negatively regulate regulatory T cell development and maintenance of peripheral CD4+ T cells in vivo. J Immunol 190 5057. PMID: 23576681.

Do you know of a great paper that uses RepSox from Tocris? If so please let us know.

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Keywords: RepSox, supplier, potent, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK5, ALK, Receptors, Activin, Receptor-like, Kinase, Serine/Threonine, Kinases, RSTKs, Transforming, Growth, Factors, Beta, stem, cells, SJN2511, ALK, 5, inhibitor, II, RepSox, SJN2511, E-616452, SJN2511, Tocris Bioscience, TGF-β Receptor Inhibitor products

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