受注:045-509-1970 |
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Synonyms | BAY2353, Niclocide, NSC 178296 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C13H8Cl2N2O4 |
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分子量 | 327.12 | CAS No. | 50-65-7 | |
Solubility (25°C)* | 体外 | 4-Methylpyridine | 20 mg/mL warmed with 50ºC water bath (61.13 mM) | |
DMSO | 4 mg/mL warmed with 50ºC water bath (12.22 mM) | |||
Water | 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. |
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). |
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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] |
キナーゼアッセイ | Protein Kinase profiling assay | |
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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 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. |
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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 |
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]
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 |
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 |
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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