Niclosamide

Catalog No.S3030 Batch:S303002

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Technical Data

Formula

C13H8Cl2N2O4
Molecular Weight 327.12 CAS No. 50-65-7
Solubility (25°C)* In vitro DMSO 4 mg/mL (12.22 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).
Targets
STAT3 [1]
(in Hela cells)
0.7 μM
In vitro 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. [1] Niclosamide is able to inhibit SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV. [2] 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. [3] 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. [4]
In vivo Niclosamide(40 mg/kg/d, i.p.) inhibits growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors. [4]

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Cell Assay:

[1]
  • Cell lines

    Hela, A549, Du145, HT-29, A431, PC3 cells

  • Concentrations

    16 μM

  • Incubation Time

    72 hours

  • Method

    Cells are plated in 96-well culture plates with cell density of 3-4 × 103 cells/well and treat with Niclosamide by adding 100 μL medium containing Niclosamide of various concentrations on the second day. After 72-hour's treatment, MTT is added to each well and incubated for additional 4-5 hours, and the absorbance is measured on a microplate reader at 570nm. Cell growth inhibition is evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 3 independent experiments.
Animal Study:

[4]
  • Animal Models

    nude mice bearing HL-60 xenograft tumors.

  • Dosages

    40 mg/kg

  • Administration

    Intraperitoneal injection

Customer Product Validation

Data from [Data independently produced by , , Acta Pharm Sin B, 2018, 8(6):889-899]

Data from [Data independently produced by , , Neoplasia, 2018, 20(10):1008-1022]

Data from [Data independently produced by , , Neoplasia, 2015, 17(7):586-97]

Data from [Data independently produced by , , Int Immunopharmacol, 2016, 36:199-204.]

Selleck's Niclosamide has been cited by 47 publications

Intravenous Injection of Na Ions Aggravates Ang II-Induced Hypertension-Related Vascular Endothelial Injury by Increasing Transmembrane Osmotic Pressure [ Int J Nanomedicine, 2023, 18:7505-7521] PubMed: 38106448
Advanced glycation end products regulate the receptor of AGEs epigenetically [ Front Cell Dev Biol, 2023, 11:1062229] PubMed: 36866277
Interleukin-29 Accelerates Vascular Calcification via JAK2/STAT3/BMP2 Signaling [ J Am Heart Assoc, 2023, 12(1):e027222] PubMed: 36537334
Androgen receptor-dependent regulation of metabolism in high grade bladder cancer cells [ Sci Rep, 2023, 13(1):1762] PubMed: 36720985
Direct-Current Electrical Field Stimulation of Patient-Derived Colorectal Cancer Cells [ Biology -Basel), 2023, 12(7)1032] PubMed: 37508461
Solamargine induces apoptosis of human renal carcinoma cells via downregulating phosphorylated STAT3 expression [ Oncol Lett, 2023, 26(5):493] PubMed: 37854861
Solamargine induces apoptosis of human renal carcinoma cells via downregulating phosphorylated STAT3 expression [ Oncol Lett, 2023, 26(5):493] PubMed: 37854861
Niclosamide is a potential candidate for the treatment of chemo-resistant osteosarcoma [ Genet Mol Biol, 2023, 46(1):e20220136] PubMed: 36735625
TFF3 promotes clonogenic survival of colorectal cancer cells through upregulation of EP4 via activation of STAT3 [ Transl Cancer Res, 2023, 12(6):1503-1515] PubMed: 37434683
Ectopic JAK-STAT activation enables the transition to a stem-like and multilineage state conferring AR-targeted therapy resistance [ Nat Cancer, 2022, 3(9):1071-1087] PubMed: 36065066

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.