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.
| 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
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
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