化合物ME0328 T6578

Product Introduction
Bioactivity


英文名: ME0328

描述: ME0328 是一种有效的选择性 PARP 抑制剂，对 PARP3 的 IC50 为 0.89 μM。

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)

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (186.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | poly ADP ribose polymerase | ME 0328 | ME-0328 | ME0328 | PARP | Inhibitor

相关产品: PARP7-IN-16 | BGP-15 | Euchrestaflavanone B | Lerzeparib | Kuguaglycoside C | PARP7-IN-15 | VEGFR/PARP-IN-1 | PI-1840 | PARP1-IN-5 dihydrochloride  | 5,​7,​4'-​Trimethoxyflavone

相关库: Anti-Aging Compound Library | Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | DNA Damage & Repair Compound Library | Anti-Pancreatic Cancer Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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