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Niclosamide is an inhibitor of the STAT3 signaling pathway; inhibits the activation, nuclear translocation and transactivation of STAT3. Niclosamide displays selectivity for STAT3 over STAT1, STAT5, JAK1, JAK2 and Src kinases. It inhibits the transcription of STAT3 target genes and induces cell growth inhibition, apoptosis and cell cycle arrest of cancer cells with constitutively active STAT3. It also reversibly inhibits mTORC1 signaling and stimulates autophagy in vitro; displays antineoplastic effects in acute myelogenous leukemia (AML) stem cells. In addition, niclosamide inhibits SARS-CoV-2 replication in vitro (IC50 = 0.34 μM in Vero E6 plaque assay) through suppression of TMEM16F activity.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 325.99. 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|
|0.25 mM||12.27 mL||61.35 mL||122.7 mL|
|1.25 mM||2.45 mL||12.27 mL||24.54 mL|
|2.5 mM||1.23 mL||6.14 mL||12.27 mL|
|12.5 mM||0.25 mL||1.23 mL||2.45 mL|
References are publications that support the biological activity of the product.
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: 24900231
Braga et al (2021) Drugs that inhibit TMEM16 proteins block SARS-CoV-2 spike-induced syncytia. Nature 594 88 PMID: 33827113
If you know of a relevant reference for Niclosamide, please let us know.
Keywords: Niclosamide, Niclosamide supplier, STAT3, mTORC1, signaling, signalling, pathway, inhibitors, inhibits, anthelmintic, SARS-CoV-2, spike, TMEM16F, STAT, mTOR, Stem, Cell, Signaling, Autophagy, Cancer, Cells, Coronavirus, Ca2+-Activated, Chloride, Channels, 4079, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Niclosamide include:
Natarajan et al (2014) STAT3 modulation to enhance motor neuron differentiation in human neural stem cells. PLoS One 9 e100405 PMID: 24945434
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