RepSox

Tocris Bioscience a Bio-Techne Brand

Catalog # 3742

Citations (6)

(1)

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Key Product Details

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)
Molecular Weight:	287.32

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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). 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 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	17.40 mL	34.80 mL
5 mM	0.70 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	0.70 mL

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References for RepSox

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

Li Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. Cell Stem Cell 2009 PMID: 19097958
Ichida A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 2009 PMID: 19818703
Gellibert Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-γ type I receptor inhibitors. J.Med.Chem. 2004 PMID: 15317461

Citations for RepSox (6)

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Citations are publications that use Bio-Techne 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
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
Mou et al. (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell. 19:217
PMID: 27320041
Lichtenberger et al. (2016) Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages. Nat Commun. 7:10537
PMID: 26837596
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

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Customer Reviews for RepSox (1)

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RepSox's ability to alter certain genes

Name: Anonymous

Species: Mouse

Assay Type: In Vivo

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.

PMID: 26837596

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Product Documents for RepSox

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.