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Submit ReviewML 171
Description: Selective NADPH oxidase 1 (NOX1) inhibitor
Chemical Name: 2-Acetylphenothiazine
Purity: ≥98% (HPLC)
Biological Activity 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.
Technical Data for ML 171
| M. Wt | 241.31 |
| Formula | C14H11NOS |
| Storage | Store at +4°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for ML 171
References for ML 171
References are publications that support the biological activity of the product.
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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Keywords: ML 171, ML 171 supplier, ML171, NADPH, oxidases, 1, NOX1, reactive, oxygen, species, ROS, inhibits, inhibitors, selective, cell, permeable, Oxidase, 4653, Tocris Bioscience
4 Citations for ML 171
Citations are publications that use Tocris products. Selected citations for ML 171 include:
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
Reviews for ML 171
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ML171 inhibits platelet aggregation and ROS production.
By
Renato Gaspar on 05/07/2019
Assay Type: Ex Vivo
Species: Human
Cell Line/Tissue: 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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