1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENiclosamideCat. No.: HY-B0497CAS No.: 50-65-7Synonyms: BAY2353分式: CHClNO分量: 327.12作靶點: STAT作通路: JAK/STAT Signaling; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMF : 9.42 mg/mL (2

2、8.80 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0570 mL 15.2849 mL 30.5698 mL5 mM 0.6114 mL 3.0570 mL 6.1140 mL10 mM 0.3057 mL 1.5285 mL 3.0570 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Niclosamide (BAY2353)種服物可利的氯化楊酰苯胺，具有驅和潛在的抗腫瘤活

3、性。Niclosamide (BAY2353) 可抑制STAT3，在 HeLa 細胞中IC50 0.25 M，并在細胞試驗中抑制 DNA 復制。IC50 & Target STAT30.25 M (IC50, in HeLa cells)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Niclosamide is an inhibitor of STAT3, inhibiting STAT3-mediated luciferase reporter activity with an IC50 of0.25 M in HeLa cell

4、s. Niclosamide (1 M) inhibits the EGF-induced nuclear translocation of STAT3 in Du145cells. Niclosamide ( 1. Niclosamide can block SARS-CoV replication at a micromolar concentration in VeroE6 cells infected with SARS-CoV 2. Niclosamide ( 3. Niclosamide inhibits the TNF-induced NF-B reporteractivity

5、in a dose- and time-dependent manner in U2OS cells. Niclosamide (125 nM) inhibits NF-B activationinduced by p65, IKK, IKK, IKK, and TAK1 in U2OS cells. Niclosamide ( 4.體內研究 Niclosamide (40 mg/kg/d, i.p.) suppresses the growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors 4.PRO

6、TOCOLKinase Assay 1 All of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusionproteins or His-tagged proteins. A radiometric protein kinase assay is used for measuring the kinase activityof the 22 protein kinases. Briefly, for each protein kinase, 50 L

7、 reaction cocktail containing 60 mM HEPES-NaOH, 3 mM MgCl2, 3 mM MnCl2, 3 M Na-orthovanadate, 1.2 mM DTT, 50 g/mL PEG20000, 1 M -33P-ATP, Niclosamide, adequate amount of enzyme and its substrate. The PKC-alpha assay additionallycontain 1 mM Ca2, 4 mM EDTA, 5 g/mL phosphatidylserine and 1 g/mL 1, 2-D

8、ioleyl-glycerol. The reactioncocktails are incubated at 37C for 60 minutes and stop with 50 L 2% (v/v) H3PO4. Incorporation of 33Pi isdetermined with a microplate scintillation counter. The activities and the IC50 values are calculated usingQuattro Workflow V2.28.MCE has not independently confirmed

9、the accuracy of these methods. They are for reference only.Cell Assay 1 Cells are plated in 96-well culture plates with cell density of 3-4 103 cells/well and treat with Niclosamide byadding 100 L medium containing Niclosamide of various concentrations on the second day. After 72-hourstreatment, MTT

10、 is added to each well and incubated for additional 4-5 hours, and the absorbance ismeasured on a microplate reader at 570 nm. Cell growth inhibition is evaluated as the ratio of theabsorbance of the sample to that of the control. The results are representative of at least 3 independentexperiments.M

11、CE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Male 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-oldAdministration 4 mice. Tumors are measured every other day with use of calipers. Mice bear

12、ing HL-60 xenografts arerandomized to receive treatment with normal saline (control) or p-niclosamide for 15 days (n=7 animalseach). Tumor volumes are calculated by the following formula: a2b0.4, where a is the smallest diameterand b is the diameter perpendicular to a. After mice are euthanized, xen

13、ografts are dissected, weighed, orpreserved.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發表的科研獻 Cell Syst. 2018 Apr 25;6(4):424-443.e7. Patent. US20180263995A1.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESee more customer validations on HYP

14、ERLINK / www.MedChemEREFERENCES1. Ren, X., et al., Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Medicinal ChemistryLetters, 2010. 1(9): p. 454-459.2. Wu CJ, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclos

15、amide. 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-kappaBpathway and generation of reactive oxygen species. Cancer R