ML 171

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Cat.No. 4653 - ML 171 | C14H11NOS | CAS No. 6631-94-3
Description: Selective NADPH oxidase 1 (NOX1) inhibitor
Chemical Name: 2-Acetylphenothiazine
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews (1)
Literature (3)

Biological Activity

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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.13 100

Preparing Stock Solutions

The following data is based on the product molecular weight 241.31. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.14 mL 20.72 mL 41.44 mL
5 mM 0.83 mL 4.14 mL 8.29 mL
10 mM 0.41 mL 2.07 mL 4.14 mL
50 mM 0.08 mL 0.41 mL 0.83 mL

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References

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

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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