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Postion:Product Catalog >API>Antiparasitic drugs>Antimalarial drug>Niclosamide
Niclosamide
  • Niclosamide
  • Niclosamide

Niclosamide NEW

Price $8 $6 $1
Package 1KG 25KG 100KG
Min. Order: 1KG
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-29

Product Details

Product Name: Niclosamide CAS No.: 50-65-7
Min. Order: 1KG Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/29
Lead time: In stock, ready for shipment Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
CCOA, MSD: Available, contact us for details Name: Sun

 1. Materials information

Names

Nameniclosamide
SynonymMore Synonyms

 Niclosamide Biological Activity

DescriptionNiclosamide is an inhibitor of STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Related Catalog
Signaling Pathways >> JAK/STAT Signaling >> STAT
Signaling Pathways >> Stem Cell/Wnt >> STAT
Research Areas >> Infection
Target

STAT3:0.25 μM (IC50, in HeLa cells)

In VitroNiclosamide is an inhibitor of STAT3, inhibiting STAT3-mediated luciferase reporter activity with an IC50 of 0.25 μM in HeLa 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) induces G0/G1 arrest and apoptosis of Du145 cancer cells in a dose dependent manner[1]. Niclosamide can block 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) causes decrease in TNF-induced NF-κB-dependent gene products involved in cell survival in HL-60 cells. Niclosamide also 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 VivoNiclosamide (40 mg/kg/d, i.p.) suppresses the growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors[4].
Kinase AssayAll of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusion proteins or His-tagged proteins. 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 Ca2, 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 AssayCells 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 570 nm. 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 AdminMale nu/nu BALB/c mice are used in the assay. HL-60 cells are inoculated s.c. on the flanks of 4- to 6-wk-old mice. Tumors are measured every other day with use of calipers. Mice bearing HL-60 xenografts are randomized to receive treatment with normal saline (control) or p-niclosamide for 15 days (n=7 animals each). Tumor volumes are calculated by the following formula: a2×b×0.4, where a is the smallest diameter and b is the diameter perpendicular to a. After mice are euthanized, xenografts are dissected, weighed, or preserved.
References

[1]. Ren, X., et al., Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Medicinal Chemistry Letters, 2010. 1(9): p. 454-459.

[2]. Wu CJ, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother. 2004 Jul;48(7):2693-6.

[3]. Chen, M., et al., The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling. Biochemistry, 2009. 48(43): p. 10267-74.

[4]. 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): p. 2516-27.

 Chemical & Physical Properties

Density1.6±0.1 g/cm3
Boiling Point424.5±45.0 °C at 760 mmHg
Melting Point225-230oC
Molecular FormulaC13H8Cl2N2O4
Molecular Weight327.120
Flash Point210.5±28.7 °C
Exact Mass325.986115
PSA95.15000
LogP5.41
Vapour Pressure0.0±1.0 mmHg at 25°C
Index of Refraction1.709





2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


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3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

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4. Contact information

For more details, pls contact us freely.

Email address: Sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137











Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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