特長 | - With slightly better solubility properties compared to Niclosamide (Prod. No. AG-CR1-3643).
- Antihelminthic, molluscicide and trypanocidal agent that inhibits mitochondrial oxidative phosphorylation and anaerobic ATP production.
- Anticancer agent with antiproliferative activity in a broad spectrum of cancer cells. Targets and inhibits multiple signaling pathways, including STAT3, NF-kB, Wnt/β-catenin, Notch and mTORC1.
- Shown to block TNF-α-induced IκBα phosphorylation, translocation of p65 and the expression of NF-κB-regulated genes and elevates reactive oxygen species (ROS) levels.
- Promotes Frizzled1 internalization, down-regulates the expression of Dishevelled-2 protein and inhibits β-catenin stabilization.
- Inhibits mTORC1 but not mTORC2 signaling in cells maintained in nutrient-rich conditions.
- Cell permeable selective STAT3 inhibitor (IC50=0.25μM). Inhibits the activation, nuclear translocation and transactivation of STAT3. Selective over STAT1, STAT5, JAK1, JAK2 and Src kinases.
- Induces cell cycle arrest, growth inhibition, autophagy and apoptosis.
- Inhibits S100A4 (Metastasin-1)-induced metastasis in vivo.
- Inhibits androgen receptor (AR) splice variants.
- Anti-inflammatory compound.
- Quorum sensing inhibitor.
- Broad range antiviral agent that targets acidified endosomes.
- Antiobesity and antidiabetic agent. Positive allosteric neuropetide Y4 receptor ligand and increases energy expenditure and lipid metabolism through mitochondrial uncoupling.
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文献 | - The effect of sublethal concentrations of the molluscicide niclosamide on the infectivity of Schistosoma mansoni cercariae: A.M. Ghandour & G. Webbe; J. Helminthol. 49, 245 (1975)
- In vitro trypanocidal activity of the anti-helminthic drug niclosamide: K. Merschjohann & D. Steverding; Exp. Parasitol. 118, 637 (2008)
- The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling: M. Chen, et al.; Biochem. 48, 10267 (2009)
- Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling: A.D. Balgi, et al.; PLoS One 4, e7124 (2009)
- Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway: X. Ren, et al.; ACS Med. Chem. Lett. 1, 454 (2010)
- Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species: Y. Jin, et al.; Cancer Res. 70, 2516 (2010)
- Niclosamide: an established antihelminthic drug as a potential therapy against S100A4-mediated metastatic colon tumors: D.M. Helfman; J. Natl. Cancer Inst. 103, 991 (2011)
- Niclosamide induces mitochondria fragmentation and promotes both apoptotic and autophagic cell death: S.J. Park, et al.; BMB Rep. 44, 517 (2011)
- Niclosamide suppresses cancer cell growth by inducing Wnt co-receptor LRP6 degradation and inhibiting the Wnt/β-catenin pathway: W. Lu, et al.; PLoS One 6, e29290 (2011)
- Niclosamide, an old antihelminthic agent, demonstrates antitumor activity by blocking multiple signaling pathways of cancer stem cells: J.X. Pan, et al.; Chin. J. Cancer 31, 178 (2012) (Review)
- Niclosamide is a proton carrier and targets acidic endosomes with broad antiviral effects: A. Jurgeit, et al.; PLoS Pathog. 8, e1002976 (2012)
- New life for an old drug: the anthelmintic drug niclosamide inhibits Pseudomonas aeruginosa quorum sensing: F. Imperi, et al.; Antimicrob. Agents Chemother. 57, 996 (2013)
- The anthelmintic drug niclosamide induces apoptosis, impairs metastasis and reduces immunosuppressive cells in breast cancer model: T. Ye, et al.; PLoS One 9, e85887 (2014)
- Multi-targeted therapy of cancer by niclosamide: A new application for an old drug: Y. Li, et al.; Cancer Lett. 349, 8 (2014) (Review)
- Niclosamide inhibits androgen receptor variants expression and overcomes enzalutamide resistance in castration-resistant prostate cancer: C. Liu, et al.; Clin. Cancer Res. 20, 3198 (2014)
- Niclosamide ethanolamine-induced mild mitochondrial uncoupling improves diabetic symptoms in mice: H. Tao, et al.; Nat. Med. 20, 1263 (2014)
- Niclosamide inhibits the inflammatory and angiogenic activation of human umbilical vein endothelial cells: M. Huang, et al.; Inflamm. Res. 64, 1023 (2015)
- Discovery of small-molecule modulators of the human Y4 receptor: G. Sliwoski, et al.; PLoS One 11, e0157146 (2016)
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