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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)
Biological Activity for RepSox
RepSox is a 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). RepSox is 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.
RepSox synthesized to Ancillary Material Grade also available.
For more information about how RepSox may be used, see our protocols: Highly Efficient Generation of CiPSCs from MEFs, Generation of β cells from hPSCs, Reprogramming MEFs into Skeletal Muscle Progenitors.
Compound Libraries for RepSox
RepSox is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for RepSox
| 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 for RepSox
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.73 | 100 | |
| ethanol | 5.75 | 20 |
Preparing Stock Solutions for RepSox
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 for RepSox
References for RepSox
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.
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9 Citations for RepSox
Citations are publications that use Tocris products. Selected citations for RepSox include:
Peter D et al (2022) Preventing VEGF-Mediated Vascular Permeability by Experimentally Potentiating BBB Characteristics in Endothelial Cells. Methods Mol Biol 2475 259-274 PMID: 35451764
Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041
Yusuke et al (2023) Generation of induced pluripotent stem cell-derived beta-cells in blood amino acids-like medium. Biol Open 12 PMID: 36811942
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
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
Alon et al (2015) Differential TGF-β Signaling in Glial Subsets Underlies IL-6-Mediated Epileptogenesis in Mice. J Immunol 195 1713-22 PMID: 26136430
Lichtenberger et al (2016) Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages. Nat Commun 7 10537 PMID: 26837596
Yung et al (2019) Sufu- And Spop-mediated downregulation of Hedgehog signaling promotes beta cell differentiation through organ-specific niche signals. Nat.Commun. 10 4647 PMID: 31604927
Do you know of a great paper that uses RepSox from Tocris? Please let us know.
Reviews for RepSox
Average Rating: 5 (Based on 1 Review.)
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RepSox's ability to alter certain genes.
By
Anonymous on 06/29/2020
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: skin
Mice received a dose of 1 μmol RepSox or vehicle only topically onto the back skin.
Mouse primary fibroblasts also treat with RepSox 25 μM.
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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
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 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
