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MPO-IN-28

MPO-IN-28

产品编号 T5340   CAS 37836-90-1

MPO-IN-28 是髓过氧化物酶 (MPO) 抑制剂,IC50=44 nM。

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MPO-IN-28 Chemical Structure
MPO-IN-28, CAS 37836-90-1
规格 价格/CNY 货期 数量
1 mg ¥ 372 现货
2 mg ¥ 498 现货
5 mg ¥ 747 现货
10 mg ¥ 1,230 现货
25 mg ¥ 2,080 现货
50 mg ¥ 3,130 现货
100 mg ¥ 4,480 现货
200 mg ¥ 6,330 现货
1 mL * 10 mM (in DMSO) ¥ 1,320 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: MPO-IN-28 (T5340)
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纯度: 99.02%
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生物活性
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参考文献
产品描述 MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.
靶点活性 MPO:44 nM (cell free)
体外活性 5 μM of MPO-IN-28 was added to MPO in the presence of 30 μM of guaiacol. In the absence of H2O2, there was no inhibition of MPO, clearly underlining that MPO-IN-28 is an irreversible mechanism-based inhibitor. MPO-IN-28 inhibits the growth of normal human dermal fibroblast (NHDF) at a concentration (IC50) of 17 μM, which is about 400 times higher than the concentration of the MPO inhibitory effect (0.044 μM).
激酶实验 The assay is based on the production of taurine chloramine produced by the MPO/H2O2/Cl? system in the presence of a selected inhibitor at defined concentration. The reaction mixture contained the following reagents in a final volume of 200 μL: 10 mM phosphate buffer (pH 7.4, 300 mM NaCl), 15 mM taurine, compound to be tested (up to 20 μM), and a fixed amount of recombinant MPO (6.6 μL of MPO batch solution diluted 2.5 times, 40 nM). When necessary, the volume was adjusted with water. This mixture was incubated at 37 °C, and the reaction was initiated with 10.0 μL of H2O2 (100 μM). After 5 min, the reaction was stopped by the addition of 10 μL of catalase (8 units/μL). To determine the amount of taurine chloramine produced, 50 μL of 1.35 mM solution of thionitrobenzoic acid was added and the volume was adjusted to 300 μL with water. Then the absorbance of the solutions was measured at 412 nm with a microplate reader, and the curve of absorbance as a function of inhibitor concentration was plotted. IC50 values were then determined by standard procedures by taking into account the absence of hydrogen peroxide as 100% inhibition and the absence of inhibitors as 0% inhibition.
细胞实验 To evaluate whether selected compounds exhibited toxicity at the cellular level at concentrations ranging from 0.005 to 50 μM, the colorimetric assay MTT was performed58 in normal human dermal fibroblasts (NHDF). Briefly, cell line was cultured in cell culture flasks, grown, and maintained at 37 °C, 95% humidity, 5% CO2 in fibroblast medium FBM supplemented with 2% fetal bovine serum, 0.1% insulin, rhFGF-B, and gentamicin and amphotericin. NHDF cells were chemically detached with trypsin and seeded in 96-well plates and left to attach for 24 h. Prior to treatment, compounds were dissolved in DMSO at a concentration of 10 mM, and cells were treated with the different concentrations of the compounds diluted in culture medium (5 nM to 50 μM) or left untreated for 72 h. The amount of viable cells was determined through the MTT mitochondrial reduction into formazan by living cells according to previously described.58 The optical density (OD) was measured in a Biorad 680RX plate reader at 570 nm (reference 630 nm), and the OD of the untreated control was normalized as 100% of viable cells, allowing determination of the concentration that inhibited their growth by 50% (IC50).
分子量 231.25
分子式 C11H13N5O
CAS No. 37836-90-1

存储

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

溶解度

DMSO: 22.73 mg/mL (98.29 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3243 mL 21.6216 mL 43.2432 mL 108.1081 mL
5 mM 0.8649 mL 4.3243 mL 8.6486 mL 21.6216 mL
10 mM 0.4324 mL 2.1622 mL 4.3243 mL 10.8108 mL
20 mM 0.2162 mL 1.0811 mL 2.1622 mL 5.4054 mL
50 mM 0.0865 mL 0.4324 mL 0.8649 mL 2.1622 mL

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TargetMol Library Books参考文献

1. Soubhye J, et al. Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J Med Chem. 2017 Aug 10;60(15):6563-6586.
GPX4-IN-4 Glutathione Peroxidase AZD5904 4-Methylesculetin NBDHEX Cefdinir N-Acetyl lysyltyrosylcysteine amide acetate 4-Aminosalicylic acid

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 经典已知活性库 代谢化合物库 NO PAINS 化合物库 抗衰老化合物库 谷氨酰胺代谢化合物库 抗代谢疾病化合物库 抗氧化化合物库 共价抑制剂库 氧化还原化合物库

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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。

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Keywords

MPO-IN-28 37836-90-1 Metabolism Glutathione Peroxidase inhibit Inhibitor MPOIN28 MPO IN 28 inhibitor

 

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