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Submit ReviewML 171
说明： Selective NADPH oxidase 1 (NOX1) inhibitor
化学名： 2-Acetylphenothiazine
纯度： ≥98% (HPLC)
生物活性 for ML 171
NADPH oxidase 1 (NOX1) inhibitor; blocks NOX1-dependent ROS generation (IC50 = 0.25 μM in a HEK293-NOX1 recombinant cell system). Selective for NOX1 over other NADPH oxidases (IC50 values are > 3 μM). Inhibits SrcYF-induced invadopodia formation in human DLD1 colon cancer cells.
技术数据 for ML 171
| 分子量 | 241.31 |
| 公式 | C14H11NOS |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 6631-94-3 |
| PubChem ID | 81131 |
| InChI Key | JWGBOHJGWOPYCL-UHFFFAOYSA-N |
| Smiles | CC(C1=CC2=C(C=C1)SC3=CC=CC=C3N2)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for ML 171
参考文献 for ML 171
参考文献是支持产品生物活性的出版物。
Gianni et al (2010) A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells. ACS Chem.Biol. 5 981 PMID: 20715845
Drummond et al (2011) Combating oxidative stress in vascular disease: NADPH oxidases as therapeutic targets. Nat.Rev.Drug Discov. 10 453 PMID: 21629295
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关键词: ML 171, ML 171 supplier, ML171, NADPH, oxidases, 1, NOX1, reactive, oxygen, species, ROS, inhibits, inhibitors, selective, cell, permeable, Oxidase, 4653, Tocris Bioscience
4 篇 ML 171 的引用文献
引用文献是使用了 Tocris 产品的出版物。 ML 171 的部分引用包括：
Cheung et al (2016) Opposing effects of TIGAR- and RAC1-derived ROS on Wnt-driven proliferation in the mouse intestine. Anal Bioanal Chem 30 52 PMID: 26679840
Hood et al (2016) Nicotinamide Adenine Dinucleotide Phosphate Oxidase-Mediated Redox Signaling and Vascular Remodeling by 16α-Hydroxyestrone in Human Pulmonary Artery Cells: Implications in Pulmonary Arterial Hypertension. Hypertension 68 796 PMID: 27402919
Moon et al (2016) NOX4-dependent fatty acid oxidation promotes NLRP3 inflammasome activation in macrophages. Nat Med 22 1002 PMID: 27455510
Shen et al (2016) Cambogin exerts anti-proliferative and pro-apoptotic effects on breast adenocarcinoma through the induction of NADPH oxidase 1 and the alteration of mitochondrial morphology and dynamics. Oncotarget 7 50596 PMID: 27418140
ML 171 的评论
平均评分: 5 (Based on 1 Review.)
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ML171 inhibits platelet aggregation and ROS production.
By
Renato Gaspar on 05/07/2019
分析类型： Ex Vivo
种属： Human
细胞系/组织： Platelets
ML171 was incubated with platelets isolated from blood. Briefly, blood was collected by brachial venipuncture into a syringe containing 4% (w/v) sodium citrate followed by addition of acid citrate dextrose (ACD: 2.5% sodium citrate, 2% D-glucose and 1.5% citric acid). Washed platelets (WP) were prepared by series of centrifugation: 100 g for 20 minutes at 22°C, and two centrifugations at 1000 g for 10 minutes to pellet the platelets in the presence of 1.25μg/mL prostacyclin (PGI2). Platelets were then resuspended in modified Tyrode’s-HEPES buffer, (20mM N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid, 5mM glucose, 134mM NaCl, 0.34mM Na2HPO4, 2.9mM KCl, 12mM NaHCO3,, and 1mM MgCl2, pH 7.3) and rested for 30 minutes at 30°C before experiments.For platelet aggregation studies, WP were incubated with increasing concentrations of ML171 for 10 minutes at 37°C and platelets stimulated with Collagen. Aggregation traces were recorded using a Helena 4-channel aggregometer.For reactive oxygen species (ROS) measurement, platelets were incubated with dihydroethidium (DHE) for 15 minutes, followed by incubation of ML171 at 3 uM for 10 minutes at 37°C. Fluorescence was recorded using a BD Accuri flow cytometer and measurements adjusted for % of resting control. Data is summary of 5 independent repeats.
Yields a yellow color liquid when dissolved in DMSO. Good stability if frozen.
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