Catalog No.S3030 Synonyms: Niclocide
Molecular Weight(MW): 327.12
Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of 0.7 μM in a cell-free assay.
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Bacterial infection in IPEC-J2 cells. The invasion and attachment of EHECO157:H7 was increased in the IPEC-J2 cells in the presence of 1 μM niclosamide. Data are expressed as the mean ± SEM (n= 6). Differences between groups were determined by paired samples t-test. *P<0.05 compared with the control.
Int Immunopharmacol, 2016, 36:199-204.. Niclosamide purchased from Selleck.
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|Description||Niclosamide can inhibit DNA replication and inhibit STAT with IC50 of 0.7 μM in a cell-free assay.|
Niclosamide (< 5 μM) dose dependently inhibits STAT3-mediated luciferase reporter activity with IC50 of 0.25 μM in HeLa cells. Niclosamide(< 2 μM) dose dependently inhibits the phosphorylation of STAT3 in Du145 cells. Niclosamide (1 μM) inhibits the EGF-induced nuclear translocation of STAT3 in Du145 cells. Niclosamide(< 2 μM) dose dependently inhibits the transcription of STAT3 downstream genes in Du145 cells. Niclosamide(< 10 μM) dose dependently induces G0/G1 arrest and apoptosis of Du145 cancer cells.  Niclosamide is able to inhibit SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV.  Niclosamide(< 7.5 μM) promotes Frizzled1 endocytosis, downregulates Dishevelled-2 protein, and inhibits Wnt3A-stimulated beta-catenin stabilization and LEF/TCF reporter activity in U2OS cells.  Niclosamide inhibits the TNF-induced NF-κB reporter activity in a dose- and time-dependent manner in U2OS cells. Niclosamide(125 nM) inhibits NF-κB activation induced by p65, IKKα, IKKβ, IKKγ, and TAK1 in U2OS cells. Niclosamide(< 500 nM) completely block the time- and dose-dependent TNFα-induced alteration of the NF-κB–DNA complex in HL-60 cells. Niclosamide(< 10 nM) inhibits constitutive NF-κB activation in U266 cells. Niclosamide inhibits TNF-induced degradation of IκBα and relocation of p65 in a dose- and time-dependent manner in HL-60, Molm13, or AML primary cells. Niclosamide(500 nM) decreases TNF-induced NF-κB–dependent gene products involved in cell survival in HL-60 cells. Niclosamide dose dependently inhibits the growth and induces robust apoptosis of AML cells associated with decreased Mcl-1 and XIAP levels and increased intracellular ROS levels. 
|In vivo||Niclosamide(40 mg/kg/d, i.p.) inhibits growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors. |
Protein Kinase profiling assay:Assay for 22 different proteins kinases is carried out by ProQinase Gmbh. All of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusion proteins or His-tagged proteins. Protein kinases are purified by affinity chromatography using either GSH-agarose or Ni_NTH-agarose. A radiometric protein kinase assay is used for measuring the kinase activity of the 22 protein kinases. Briefly, for each protein kinase, 50 μL reaction cocktail containing 60 mM HEPES-NaOH, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/mL PEG20000, 1 μM [γ-33P]-ATP, Niclosamide, adequate amount of enzyme and its substrate. The PKC-alpha assay additionally contain 1 mM Cacl2, 4 mM EDTA, 5 μg/mL phosphatidylserine and 1 μg/mL 1, 2-Dioleyl-glycerol. The reaction cocktails are incubated at 37 °C for 60 minutes and stop with 50 μL 2% (v/v) H3PO4. Incorporation of 33Pi is determined with a microplate scintillation counter. The activities and the IC50 values are calculated using Quattro Workflow V2.28.
|In vitro||DMF||12 mg/mL (36.68 mM) warming|
|In vivo||1% DMSO+30% polyethylene glycol+1% Tween 80||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02807805||Not yet recruiting||Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer||University of California, Davis|National Cancer Institute (NCI)||October 2016||Phase 2|
|NCT02687009||Not yet recruiting||Colon Cancer||Michael Morse, MD|Duke University||July 2016||Phase 1|
|NCT02532114||Recruiting||Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Adenocarcinoma||University of Washington|National Cancer Institute (NCI)||December 2015||Phase 1|
|NCT02519582||Not yet recruiting||Colorectal Cancer||Charite University, Berlin, Germany|Center for Molecular Medicine||August 2015||Phase 2|
|NCT01296958||Completed||Taenia Solium Taeniasis||Oregon Health and Science University|Universidad Nacional Mayor de San Marcos|National Institute of Neurological Disorders and Stroke (NINDS)||May 2011||--|
|NCT00138359||Terminated||Intestinal Parasitism||National Institute of Allergy and Infectious Diseases (NIAID)||December 2004||--|
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