Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SGI-1027 (DNA Methyltransferase Inhibitor II) 是一种 DNA 甲基转移酶(DNMT)抑制剂,对以 poly(dI-dC) 为底物的 DNMT3B,DNMT3A 和 DNMT1 的IC50值分别为 7.5 μM,8 μM 和 12.5 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 215 | 现货 | ||
5 mg | ¥ 513 | 现货 | ||
10 mg | ¥ 898 | 现货 | ||
25 mg | ¥ 1,610 | 现货 | ||
50 mg | ¥ 2,860 | 现货 | ||
100 mg | ¥ 4,160 | 现货 | ||
500 mg | ¥ 8,750 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 572 | 现货 |
产品描述 | SGI-1027 (DNA Methyltransferase Inhibitor II) is an effective and selective inhibitor of DNA methyltransferase (DNMT). The IC50 of SGI-1027(SGI1027) against DNMT1, DNMT3A, and DNMT3B are 6, 8, 7.5 μM, respectively. |
靶点活性 | DNMT3B:7.5 μM, DNMT3A:8 μM, DNMT1:6 μM |
体内活性 | 在U937人白血病细胞系中,SGI-1027(0-100 μM)显示出适度的促凋亡作用,单不影响细胞周期。SGI-1027可直接抑制DNMTs使DNA甲基化受到抑制,并使各种人癌细胞系中的DNMT1选择性降解。在大鼠肝癌H4IIE细胞中,SGI-1027毒性很小或没有。 |
激酶实验 | DNA methyltransferase (CpG methyltransferase) assay: DNA methylase activity is assayed by measuring the incorporation of 3H1-methyl group from Ado-Met into DNA using DE-81 ion exchange filter binding assay with some modifications. Human recombinant DNMT1, recombinant mouse Dnmt3a/ Dnmt3b (500 ng) is incubated with 500 ng of poly(dI-dC) or hemimethylated DNA duplex and 75 or 150 nM (0.275μCi or 0.55μCi) of [methyl-3H]-Sadenosylmethionine (Ado-Met) in a total volume of 50 μl at 37°C for 1hr. or M. Sss I is assayed in the supplier's buffer. SGI-1027 or decitabine is added at indicated concentrations. Each reaction is performed in duplicate and included controls with no inhibitor or no DNA. The reaction is stopped by soaking reaction mixture onto a Whatman DE-81 ion exchange filter disc, washed (five times, 10 min each, with 0.5M Na-phosphate buffer; pH 7.0) dried and counted in a scintillation counter. The background radioactivity (no DNA control) is subtracted from the values obtained with reaction mixtures containing DNA and the radioactivity obtained in the reaction without any inhibitor is considered as 100% activity. IC50 is determined by interpolation from the plot of percent activity versus inhibitor concentration. To determine the nature of inhibition of DNMTase activity by SGI-1027, DNMT1 enzyme activityis measured in presence of a fixed concentration of inhibitor (0, 2.5, 5, and 10 μM) while one of the two (Ado-Met or DNA) was varied in a particular reaction mixture. At a fixed concentration of DNA (500 ng) varying concentrations of Ado-Met used are from 25-500 nM, respectively. Similarly, final DNA concentrations are varied from (25-500ng) at 75 nM Ado-Met. |
细胞实验 | Rat hepatoma H4IIE cells are used as the test system. These cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48 h exposed to SGI-1027 at concentrations ranging from 0 to 300 μMol/L. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis. The half-maximal toxic concentration (TC50) is determined from the dose-response curves.(Only for Reference) |
别名 | DNA Methyltransferase Inhibitor II, SGI1027 |
分子量 | 461.52 |
分子式 | C27H23N7O |
CAS No. | 1020149-73-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 23.1 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1668 mL | 10.8338 mL | 21.6675 mL | 54.1688 mL |
5 mM | 0.4334 mL | 2.1668 mL | 4.3335 mL | 10.8338 mL | |
10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL | 5.4169 mL | |
20 mM | 0.1083 mL | 0.5417 mL | 1.0834 mL | 2.7084 mL | |
50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0834 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SGI-1027 1020149-73-8 Apoptosis Chromatin/Epigenetic DNA Methyltransferase DNA MTases inhibit SGI 1027 DNA Methyltransferase Inhibitor II SGI1027 Inhibitor DNMTs inhibitor