Importazole-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEImportazoleCat. No.: HY-101091CAS No.: 662163-81-7分式: CHN分量: 318.42作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33 mg/mL (103.64 mM)* means soluble, but saturation

2、unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1405 mL 15.7025 mL 31.4051 mL5 mM 0.6281 mL 3.1405 mL 6.2810 mL10 mM 0.3141 mL 1.5703 mL 3.1405 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适

3、当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.85 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.85 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Importazole核

4、转运受体importin-的分抑制剂。体外研究 Importazole specifically blocks importin-mediated nuclear import both in Xenopus egg extracts and culturedcells, without disrupting transportin-mediated nuclear import or CRM1-mediated nuclear export. Importazoleimpairs the release of an importin- cargo FRET probe and causes

5、both predicted and novel defects inspindle assembly 1. Importazole displays an IC50 of approximately 15 M for inhibition of NFAT-GFPimport. Importazole has an IC50 of approximately 22.5 M in HeLa cells following treatment over a 24-hourperiod 1. Importazole induces a dose-and time-dependent inhibiti

6、on of myeloma cells growth. And the IC50values of importazole on RPMI 8226 and NCI-H929 after 48 hours incubation are (4.430.41) and(4.780.35) mol/L, respectively. Treatment of RPMI 8226 and NCI-H929 cells with 8 mol/L importazole for24 h could inhibit NF-B import to nucleus and reduce its DNA bindi

7、ng activity 2.PROTOCOLCell Assay 1 HEK 293 cells stably expressing NFAT-GFP are grown on glass coverslips to approximately 50% confluencyprior to drug treatment. In all cases, importazole is used at 40 M and leptomycin B is used at 10 ng/mL. Forcontrols, DMSO is used at a concentration of 0.4%. Iono

8、mycin is added at 1.25 M. Importazole andleptomycin B treatments are all for 1 hour. In all experiments cells are fixed with 4% formaldehyde prior tofluorescence microscopy. DNA is visualized with 1 g/mL Hoechst dye. For quantification, 100 cells fromeach condition are analyzed and the percentage th

9、at shows nuclear accumulation of NFAT-GFP arecalculated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Nature. 2018 Nov;563(7729):131-136. bioRxiv. 2019 Jan.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Soderholm J

10、F, et al. Importazole, a small molecule inhibitor of the transport receptor importin-. ACS Chem Biol. 2011 Jul 15;6(7):700-8.2. Yan WQ, et al. Effect of nuclear receptor inhibitor importazole on the proliferation and apoptosis of multiple myeloma cells. ZhonghuaXue Ye Xue Za Zhi. 2013 Apr;34(4):323-6.McePdfHeightCaution: Product has not been fully vali