Biological Activity
Inhibitor of the STAT3 signaling pathway; inhibits the activation, nuclear translocation and transactivation of STAT3. Displays selectivity for STAT3 over STAT1, STAT5, JAK1, JAK2 and Src kinases. Inhibits the transcription of STAT3 target genes and induces cell growth inhibition, apoptosis and cell cycle arrest of cancer cells with constitutively active STAT3. Also reversibly inhibits mTORC1 signaling and stimulates autophagy in vitro; displays antineoplastic effects in acute myelogenous leukemia (AML) stem cells.
Technical Data
| M. Wt | 325.99 |
| Formula | C13H8Cl2N2O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 50-65-7 |
| PubChem ID | 4477 |
| InChI Key | RJMUSRYZPJIFPJ-UHFFFAOYSA-N |
| Smiles | O=C(NC2=C(Cl)C=C([N+]([O-])=O)C=C2)C1=C(O)C=CC(Cl)=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 | 3.26 | 10 | |
| ethanol | 8.15 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 325.99. 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 | 3.07 mL | 15.34 mL | 30.68 mL |
| 5 mM | 0.61 mL | 3.07 mL | 6.14 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.07 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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References
References are publications that support the products' biological activity.
Balgi et al (2009) Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4 e7124 PMID: 19771169
Jin et al (2010) Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-κB pathway and generation of reactive oxygen species. Cancer Res. 70 2516 PMID: 20215516
Ren et al (2010) Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Med.Chem.Lett. 1 454 PMID:
Keywords: Niclosamide, supplier, STAT3, mTORC1, signaling, signalling, pathway, inhibitors, inhibits, anthelmintic, STAT, mTOR, Stem, Cell, Signaling, Autophagy, Cancer, Stem, Cells, STAT, Tocris Bioscience
