RepSox

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Cat.No. 3742 - RepSox | C17H13N5 | CAS No. 446859-33-2
Description: Potent and selective inhibitor of TGF-βRI
Alternative Names: E-616452, SJN 2511, ALK5 Inhibitor II
Chemical Name: 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
Purity: ≥99% (HPLC)
Datasheet
Citations (5)
Reviews
Protocols (3)
Literature (5)
Pathways (1)

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.

Compound Libraries

RepSox is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 287.32
Formula C17H13N5
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 446859-33-2
PubChem ID 449054
InChI Key LBPKYPYHDKKRFS-UHFFFAOYSA-N
Smiles CC1=NC(C2=NNC=C2C4=NC3=CC=CN=C3C=C4)=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.73 100
ethanol 5.75 20

Preparing Stock Solutions

The following data is based on the product molecular weight 287.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.48 mL 17.4 mL 34.8 mL
5 mM 0.7 mL 3.48 mL 6.96 mL
10 mM 0.35 mL 1.74 mL 3.48 mL
50 mM 0.07 mL 0.35 mL 0.7 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

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


If you know of a relevant reference for RepSox, please let us know.

View Related Products by Product Action

View all TGF-β Receptor Inhibitors

Keywords: RepSox, RepSox supplier, potent, inhibitors, inhibits, TGF-βRI, TGF-β, TGF-betaRI, TGFbRI, TGFbR1, tgf-b1ALK5, ALK, Receptors, Receptor-like, Kinase, Serine/Threonine, Kinases, RSTKs, Transforming, Growth, Factors, Beta, stem, cells, SJN2511, 5, inhibitor, II, RepSox, E-616452, SJN251, SJN, 2511, ALK5, Inhibitor, TGF-beta, Reprogramming, 3742, Tocris Bioscience

5 Citations for RepSox

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

Segal et al (2019) Single cell analysis of human foetal liver captures the transcriptional profile of hepatobiliary hybrid progenitors. Nat Commun 10 3350 PMID: 31350390

Lichtenberger et al (2016) Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages. Nat Commun 7 10537 PMID: 26837596

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

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

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


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Reviews for RepSox

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Protocols for RepSox

The following protocols feature additional information for the use of RepSox (Cat. No. 3742).

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.

Pathways for RepSox

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.