Niclosamide

製品コードS3030 バッチS303003

印刷

化学情報

Chemical Structure Synonyms BAY2353, Niclocide, NSC 178296 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H8Cl2N2O4
分子量 327.12 CAS No. 50-65-7
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 2 mg/mL (6.11 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
10% DMSO 40% PEG 300 5%Tween80 45%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.200mg/ml (0.61mM) Taking the 1 mL working solution as an example, add 100 μL of 2 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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).
in vitro Niclosamide (< 5 μM) dose dependently inhibits STAT3-mediated luciferase reporter activity with IC50 of 0.25 μM in HeLa cells. This compound (< 2 μM) dose dependently inhibits the phosphorylation of STAT3 in Du145 cells. It (1 μM) inhibits the EGF-induced nuclear translocation of STAT3 in Du145 cells. This chemical (< 2 μM) dose dependently inhibits the transcription of STAT3 downstream genes in Du145 cells. It (< 10 μM) dose dependently induces G0/G1 arrest and apoptosis of Du145 cancer cells. [1] This compound is able to inhibit SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV. [2] It (< 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] This chemical inhibits the TNF-induced NF-κB reporter activity in a dose- and time-dependent manner in U2OS cells. It (125 nM) inhibits NF-κB activation induced by p65, IKKα, IKKβ, IKKγ, and TAK1 in U2OS cells. This compound (< 500 nM) completely block the time- and dose-dependent TNFα-induced alteration of the NF-κB–DNA complex in HL-60 cells. It (< 10 nM) inhibits constitutive NF-κB activation in U266 cells. This chemical 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. It (500 nM) decreases TNF-induced NF-κB–dependent gene products involved in cell survival in HL-60 cells. This compound 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Hela, A549, Du145, HT-29, A431, PC3 cells
濃度 16 μM
反応時間 72 hours
実験の流れ

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 this compound 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.
動物実験 動物モデル nude mice bearing HL-60 xenograft tumors.
投薬量 40 mg/kg
投与方法 Intraperitoneal injection

参考

  • http://pubs.acs.org/doi/full/10.1021/ml100146z
  • https://pubmed.ncbi.nlm.nih.gov/15215127/
  • https://pubmed.ncbi.nlm.nih.gov/19772353/
  • https://pubmed.ncbi.nlm.nih.gov/20215516/

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HIV-1 Vpu interacts with RBM10 to promote HIV-1 infection [ mSystems, 2025, 10(8):e0040325] PubMed: 40742131
Evaluation of Nano-Niclosamide in Killing Demodex folliculorum In Vitro and the Potential Application in Ocular Surface [ Pharmaceutics, 2025, 17(3)332] PubMed: 40142996
Arylsulfatase B induces melanoma apoptosis by the ubiquitin ligase COP1 [ J Biol Chem, 2025, 301(8):110402] PubMed: 40562100
Interleukin 29 is a novel antiangiogenic factor in angiogenesis [ Cytokine, 2025, 186:156850] PubMed: 39752899
TSPAN6 reinforces the malignant progression of glioblastoma via interacting with CDK5RAP3 and regulating STAT3 signaling pathway [ Int J Biol Sci, 2024, 20(7):2440-2453] PubMed: 38725860
RACK1 enhances STAT3 stability and promotes T follicular helper cell development and function during blood-stage Plasmodium infection in mice [ PLoS Pathog, 2024, 20(7):e1012352] PubMed: 39024388
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
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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