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Cat. No. Name Size Price Add Cart
KI0712Niclosamide100 mg$272

Chemical Characteristic

Product NameNiclosamide
SynonymsNiclocide, Yomesan, Bayluscide
CAS No.50-65-7
Molecular Weight 327.12
FormulaC13H8Cl2N2O4
Chemical Structure

Biological activities

Niclosamide is effective as a virus replication inhibitor. Niclosamide is an antihelminthic drug and has been used to treat tapeworm. [1] Niclosamide is a potent inducer of LC3-positive autophagosomes, an inhibitor of the Wnt/Frizzled pathway, a suppressor of the autonomous notch-signalling pathway, and an inhibitor of mTOR signaling. [2] Niclosamide is a unique small molecule Wnt/β-catenin signaling inhibitor targeting the Wnt co-receptor LRP6 on the cell surface. [3] Niclosamide inhibits replication of a newly discovered coronavirus, SARS-CoV. Niclosamide inhibits viral antigen synthesis with an IC50 ranging from 1 to 3 µM. [1]Niclosamide effectively inhibits influenza virus (strain A/Puerto Rico/8/34/H1N1 depicted PR8) with an IC50 of 0.83 µM in human lung adenocarcinoma epithelial A549 cells. Niclosamide is also an effective antiviral in non-transformed cells, including WI-38 human embryonic diploid airway cells infected with HRV1A, with an IC50 of 1.3 µM. [2] Niclosamide suppresses LRP6 expression and phosphorylation, blocks Wnt3A-induced β-catenin accumulation, and inhibits Wnt/β-catenin signaling in HEK293 cells. Niclosamide induces cancer cell apoptosis, and displays excellent anticancer activity with IC50 less than 1 µM for prostate PC-3 and DU145, breast MDA-MB-231 and T-47D cancer cells. [3] Niclosamide promotes Frizzled1 endocytosis, down-regulates Dishevelled-2 protein, and inhibits Wnt3A-stimulated β-catenin stabilization and LEF/TCF reporter activity. Niclosamide inhibits Wnt/Frizzled signaling induced by a full agonist, with an IC50 of 0.5 µM. [4] Niclosamide inhibits the transcription and DNA binding of NF-κB. Niclosamide blocks tumor necrosis factor-induced IκBα phosphorylation, translocation of p65, and expression of NF-κB-regulated genes. Niclosamide inhibits the steps TAK1閳墳κB kinase (IKK) and IKK閳墳κBα. Niclosamide also increases the levels of reactive oxygen species (ROS) in acute myelogenous leukemia (AML) cells. [5] Niclosamide decreases downstream β-catenin signaling and exerts anti-proliferative effects in human colon cancer cell lines and colorectal cancer cells isolated by surgical resection of metastatic disease, regardless of mutations in adenomatous polyposis coli (APC). [6] Niclosamide inhibits growth of xenografted AML cells in nude mice. [5] Niclosamide inhibits the growth of human colorectal cancers (CRCs) in NOD/SCID mice. [6]

Protocols

Niclosamide is prepared as a 10 mM stock solution in DMSO. [1]

References

[1] Wu CJ, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother. 2004, 48(7): 2693-2696. 閵嗏偓閵嗏偓
[2] Jurgeit A, et al. Niclosamide is a proton carrier and targets acidic endosomes with broad antiviral effects. PLoS Pathog. 2012, 8(10): e1002976. 閵嗏偓閵嗏偓
[3] Lu W, et al. Niclosamide suppresses cancer cell growth by inducing Wnt co-receptor LRP6 degradation and inhibiting the Wnt/β-catenin pathway. PLoS One. 2011, 6(12): e29290. 閵嗏偓閵嗏偓
[4] Chen M, et al. The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling. Biochemistry. 2009, 48(43): 10267-10274. 閵嗏偓閵嗏偓
[5] Jin Y, et al. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species. Cancer Res. 2010, 70(6): 2516-2527. 閵嗏偓閵嗏偓
[6] Osada T, et al. Antihelminth compound niclosamide downregulates Wnt signaling and elicits antitumor responses in tumors with activating APC mutations. Cancer Res. 2011, 71(12): 4172-4182. 閵嗏偓閵嗏偓

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