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CRT0044876

产品编号 T6456Cas号 6960-45-8
别名 7-硝基吲哚-2-甲酸, NSC 69877,7-NO2-ICA, NSC 69877, 7-Nitroindole-2-Carboxylic Acid

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。

CRT0044876
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CRT0044876

纯度: 98.98%
产品编号 T6456 别名 7-硝基吲哚-2-甲酸, NSC 69877,7-NO2-ICA, NSC 69877, 7-Nitroindole-2-Carboxylic AcidCas号 6960-45-8

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 256现货
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纯度:98.98%
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产品介绍

生物活性
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7-硝基吲哚-2-甲酸, NSC 69877,7-NO2-ICA, NSC 69877, 7-Nitroindole-2-Carboxylic Acid
化学信息
分子量206.15
分子式C9H6N2O4
CAS No.6960-45-8
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 40 mg/mL (194.03 mM)
Ethanol: 1 mg/mL (4.85 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM4.8508 mL24.2542 mL48.5084 mL242.5418 mL
DMSO
1mg5mg10mg50mg
5 mM0.9702 mL4.8508 mL9.7017 mL48.5084 mL
10 mM0.4851 mL2.4254 mL4.8508 mL24.2542 mL
20 mM0.2425 mL1.2127 mL2.4254 mL12.1271 mL
50 mM0.0970 mL0.4851 mL0.9702 mL4.8508 mL
100 mM0.0485 mL0.2425 mL0.4851 mL2.4254 mL

计算器

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体内实验配液计算器

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TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

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% DMSO
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