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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHoechst 33258 trihydrochlorideCat. No.: HY-15558ACAS No.: 23491-45-4Synonyms: bisBenzimide H 33258 trihydrochloride; H 33258trihydrochloride分式: CHClNO分量: 533.88作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -
2、80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 72.85 mg/mL (136.45 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.8731 mL 9.3654 mL 18.7308 mL5 mM 0.3746 mL 1.8731 mL 3.7462 mL10 mM 0.1873 mL 0.9365 mL 1.8731 mL請根據(jù)產(chǎn)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。BIO
3、LOGICAL ACTIVITY物活性 Hoechst 33258 trihydrochloride (bisBenzimide H 33258 trihydrochloride)種熒光染料,于 DNA 染。IC50 & Target IC50: 51.314.56 M (HeLa cell), 32.433.27 M (HL60 cell), 15.422.16 M (U937 cell) 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Hoechst 33258, a fluorescent compound with a he
4、ad-to-tail bis-benzimidazole structure, is initially found tobe cytotoxic against L1210 murine leukemia. Hoechst 33258 is evaluated for their cytotoxicity against humantumor cell lines, which are cervix carcinoma cell line (HeLa), Human promyelocytic leukemia cell (HL60) andU937 cell Line. The IC50
5、determined in the case of HeLa, HL60 and U937 is 51.314.56, 32.433.27 and15.422.16 M for Hoechst 33258, respectively 1. The cytotoxic property of Hoechst 33258 is investigatedon a panel of seven tumour cell lines of different histological origin and Madine-Darby canine kidney (MDCK)normal cells. All
6、 cell lines, except MCF-7, exposed to Hoechst 33258 exhibit GI50 from 8410-6 to 191.510-6 mol/dm3. Under the same experimental conditions, Hoechst 33258, used as a binder reference compound,stops the cell cycle in S phase and G0/G1 2.PROTOCOLCell Assay 2 Hoechst 33258 is prepared as stock solutions
7、in highly pure water. Working solutions in a concentrationrange of 10-3-10-6 mol/dm3 are prepared prior to testing. Cytotoxic effects of Hoechst 33258 on tested celllines are determined by the MTT assay. Cells are seeded in 96 micro well flat bottom plates at aconcentration of 2104 cells/mL and left
8、 overnight in the CO2 incubator allowing them to attach to the platesurface. Growing medium is replaced with compound supplemented or control medium and incubated for 72h. Fresh medium with 5 mg/mL of MTT is added onto cells and incubated for 4 h at 37C. Upon mediaremoval, water insoluble MTT-formaz
9、an crystals formed inside the living cells are dissolved in DMSO and theabsorbance at 570 nm proportional to the number of living cells is measured on an Elisa Microplate Reader.All experiments are performed at least three times in triplicates.The GI50 value, defined as the compoundconcentration (M)
10、 leading to cellular growth inhibition by 50%, is calculated and used as a parameter tocompare cytotoxicity among the compounds 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Chem Eng J. 2019 Feb. J Cell Biochem. 2018 Dec 14. Int J Bioche
11、m Cell Biol. 2017 Mar;84:75-88. Acta Biochim Biophys Sin (Shanghai). 2019 Aug 5;51(8):814-825. BIOTECHNOLOGY BULLETIN 2018, 34(12):172-178See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wang XJ, et al. Newly synthesized bis-benzimidazole derivatives exerting anti-tumor activity
12、 through inductionof apoptosis andautophagy. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6297-300.2. Stoli? I, et al. Synthesis, DNA/RNA affinity and antitumour activity of new aromatic diamidines linked by 3,4-ethylenedioxythiophene. EurJ Med Chem. 2011 Feb;46(2):743-55.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution:
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