RepSox

Pricing Availability Delivery Time Qty
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 (3)
Literature
Pathways

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.73 100
ethanol 14.37 50

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

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Reconstitution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, 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, E-616452, SJN, 2511, ALK5, Inhibitor, II, TGF-beta, Receptors, Reprogramming, TGF-beta, Receptors, Tocris Bioscience

3 Citations for RepSox

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

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

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


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

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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.

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.

Protocols

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