RepSox

Tocris Bioscience, part of Bio-Techne | Catalog # 3742

(1)

Citations (38)

COA / SDS

Potent and selective inhibitor of TGF-βRI

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

View Full Technical Details for RepSox

Technical Data
Citations / Reviews (1)

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 (see our protocols below); also used in protocols to generate CiPSCs from MEFs or β cells from hPSCs (see below); used in protocols to generate pancreatic beta cells from hPSCs or CiPSCs from MEFs. 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.

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	17.40 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