Niclosamide

Biological Activity

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.

Technical Data

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.

Background References

1. STAT3 modulation to enhance motor neuron differentiation in human neural stem cells.
   Natarajan, Rajalaxm, Singal, Vinamrat, Benes, Richard, Gao, Junling, Chan, Hoi, Chen, Haijun, Yu, Yongjia, Zhou, Jia, Wu, Ping
   PLoS ONE, 2014;9(6):e100405.
2. Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling.
   Balgi et al.
   PLoS One, 2009;4:e7124
3. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-κB pathway and generation of reactive oxygen species.
   Jin et al.
   Cancer Res., 2010;70:2516
4. Periostin Activation of Integrin Receptors on Sensory Neurons Induces Allergic Itch
   SK Mishra, JJ Wheeler, S Pitake, H Ding, C Jiang, T Fukuyama, JS Paps, P Ralph, J Coyne, M Parkington, J DeBrecht, LC Ehrhardt-H, GP Cruse, W Bäumer, RR Ji, MC Ko, T Olivry
   Cell Rep, 2020;31(1):107472.

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