Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CRT0044876 (7-NO2-ICA) 是一种高选择性的嘌呤/嘧啶核苷核酸内切酶 1 抑制剂,IC50约为 3 μM。它也是 APE1 所属的核酸外切酶 III 家族的特异性抑制剂,可抑制 APE1 的 AP 内切酶、3′-磷酸二酯酶和 3′-磷酸酶活性,可增强几种 DNA 碱基靶向化合物的细胞毒性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 243 | 现货 | ||
10 mg | ¥ 333 | 现货 | ||
25 mg | ¥ 566 | 现货 | ||
50 mg | ¥ 828 | 现货 | ||
100 mg | ¥ 1,220 | 现货 | ||
200 mg | ¥ 1,790 | 现货 | ||
500 mg | ¥ 2,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 256 | 现货 |
产品描述 | CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM. |
靶点活性 | APE1:3 μM |
体外活性 | CRT0044876 potently inhibits the AP endonuclease, 3'-phosphodiesterase and 3'-phosphatase activities of APE1, and exhibits the selectivity for the inhibition of exonuclease III family. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds with an accumulation of unrepaired AP sites. [1] CRT0044876, by inhibition of the BER pathway increases oxidative DNA damage temporally related to increased intracellular reactive oxygen species in an acidic tumor microenvironment, and thus results in cell cycle arrests and increased DNA double strand breaks, leading to cell death. [2] |
激酶实验 | AP site cleavage assay: BER reaction buffer comprises 40 mM HEPES–KOH (pH 7.8), 5 mM MgCl2, 0.5 mM DTT and 0.1 mM EDTA. A 10 μl AP site cleavage reaction comprised of BER buffer mix, purified protein (3.3 nM final concentration of APE1) and 0.75 ng reduced AP site double-stranded oligonucleotide. The mixture is incubated at 37°C for 1 h. A total of 1 μl of stop buffer (50% glycerol, 10 mM Tris–HCl, 1 mM EDTA, 0.1% bromophenol blue and 0.1% Xylene cyanol) is added, and the sample mixture is denatured at 90–100°C for 2 min. The sample is then run on a 15% TBE Criterion? Pre-Cast Gel, with electrophoresis at a constant current of 30 mA for 30 min, and the radiolabeled substrate and reaction products are visualized using a phosphorImager. The inhibitory activity of potential APE1-targeting compounds are analyzed at drug concentrations ranging from 0.1 to 100 μM. The resolved radiolabeled bands are quantified using ImageQuant software analysis, and IC50 values are calculated by determining the concentration of the inhibitor that reduced APE1 activity to 50% of the control values. |
细胞实验 | HT1080 fibrosarcoma cells are grown in 2% RPMI medium [supplemented with penicillin 0.06 g/l, streptomycin 0.1 g/l (pH 7.0), 10% fetal bovine serum and 4 mM glutamine]. Only cells with a plating efficiency of ≥60% are used for clonogenic survival analysis. Tissue culture dishes (10 cm) are seeded with 500 cells per dish and the culture is maintained in a humidified incubator at 37°C in an atmosphere of 5% CO2 and 95% air. To evaluate the toxicity profile of putative APE1 inhibitors, various concentrations (100–500 μM) of inhibitor are added to the medium, and cultures were incubated for 7-10 days until cell colonies are formed. Colonies are fixed [75% (v/v) methanol, 25% (v/v) acetic acid] for 30 min and stained with crystal violet (1 mg/ml in distilled water) for 4 h at room temperature. Visible colonies are counted on a colony counter. (Only for Reference) |
别名 | NSC 69877,7-NO2-ICA, 7-硝基吲哚-2-甲酸, NSC 69877, 7-Nitroindole-2-Carboxylic Acid |
分子量 | 206.15 |
分子式 | C9H6N2O4 |
CAS No. | 6960-45-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 39 mg/mL (189.2 mM)
Ethanol: 1 mg/mL (4.85 mM)
H2O: < 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 / Ethanol | 1 mM | 4.8508 mL | 24.2542 mL | 48.5084 mL | 121.2709 mL |
DMSO | 5 mM | 0.9702 mL | 4.8508 mL | 9.7017 mL | 24.2542 mL |
10 mM | 0.4851 mL | 2.4254 mL | 4.8508 mL | 12.1271 mL | |
20 mM | 0.2425 mL | 1.2127 mL | 2.4254 mL | 6.0635 mL | |
50 mM | 0.097 mL | 0.4851 mL | 0.9702 mL | 2.4254 mL | |
100 mM | 0.0485 mL | 0.2425 mL | 0.4851 mL | 1.2127 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。
CRT0044876 6960-45-8 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis CRT-0044876 non-toxic CRT 0044876 DNA NSC 69877,7-NO2-ICA Inhibitor base exonuclease 7-硝基吲哚-2-甲酸 inhibit NSC 69877 7-Nitroindole-2-Carboxylic Acid endonuclease NSC-69877 excision NSC69877 repair inhibitor