Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ME0328 是一种有效的选择性 PARP 抑制剂,对 PARP3 的 IC50 为 0.89 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 186 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 662 | 现货 | ||
25 mg | ¥ 1,320 | 现货 | ||
50 mg | ¥ 2,230 | 现货 | ||
100 mg | ¥ 3,360 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
靶点活性 | PARP3:0.89 μM |
体外活性 | ME0328具有溶解性,能渗透细胞,并且在人类肝微粒体和大鼠肝细胞中表现出代谢稳定性。ME0328(10 μM)通过影响A549和MRC5细胞中的ARTD3,显著延迟γH2AX-焦点的解决,而无明显的毒性。[1] |
激酶实验 | Enzymatic Assays: Protein ADP-ribosylation is measured using hexahistidine-tagged ARTD proteins and recombinant histone proteins captured on 96-well Ni2+-chelating plates (5-PRIME). ADP-ribosylation reactions are initiated by addition of NAD+ (2% biotinylated), and modified reaction products are detected by chemiluminescence. Km values are estimated using plots of initial rates vs. NAD+ concentrations and linear curve fitting with GraphPad Prism. All compounds are dissolved in dimethyl sulfoxide (DMSO) to a stock concentration of 50 mM. Experiments to determine IC50 values are conducted with compound concentrations in the range between 10 nM and 450 μM with a DMSO concentration of 1% (v/v). Measurements are carried out at an NAD+ concentration below Km for each transferase. IC50 values are estimated using curve fitting with GraphPad Prism. Reported values represent means ± SE of the fits of the curves based on duplicate or triplicate experiments, each determined based on three replicates. |
细胞实验 | Compound cytotoxicity in A549 and MRC5 cells is evaluated using WST-1 assays. A549 cells are cultured in Dulbecco’s Modified Eagle’s Medium supplemented with 10% fetal calf serum (FCS), penicillin, and streptomycin. MRC5 cells are cultured in Minimal Essential Medium supplemented with 10% FCS, penicillin, streptomycin, and l-glutamine. Both cell lines are maintained in a humidified incubator at 37°C and 5% CO2. (Only for Reference) |
分子量 | 321.37 |
分子式 | C19H19N3O2 |
CAS No. | 1445251-22-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (186.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1117 mL | 15.5584 mL | 31.1168 mL | 77.792 mL |
5 mM | 0.6223 mL | 3.1117 mL | 6.2234 mL | 15.5584 mL | |
10 mM | 0.3112 mL | 1.5558 mL | 3.1117 mL | 7.7792 mL | |
20 mM | 0.1556 mL | 0.7779 mL | 1.5558 mL | 3.8896 mL | |
50 mM | 0.0622 mL | 0.3112 mL | 0.6223 mL | 1.5558 mL | |
100 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7779 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。
ME0328 1445251-22-8 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit poly ADP ribose polymerase ME 0328 ME-0328 Inhibitor inhibitor