ML 171

Selective NADPH oxidase 1 (NOX1) inhibitor CAS# 6631-94-3

ML 171

Catalog No. BCC6252----Order now to get a substantial discount!

Product Name & Size Price Stock
ML 171: 5mg $12 In Stock
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Quality Control of ML 171

Number of papers citing our products

Chemical structure

ML 171

3D structure

Chemical Properties of ML 171

Cas No. 6631-94-3 SDF Download SDF
PubChem ID 81131 Appearance Powder
Formula C14H11NOS M.Wt 241.31
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 64 mg/mL (265.22 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-(10H-phenothiazin-2-yl)ethanone
SMILES CC(=O)C1=CC2=C(C=C1)SC3=CC=CC=C3N2
Standard InChIKey JWGBOHJGWOPYCL-UHFFFAOYSA-N
Standard InChI InChI=1S/C14H11NOS/c1-9(16)10-6-7-14-12(8-10)15-11-4-2-3-5-13(11)17-14/h2-8,15H,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ML 171

DescriptionNADPH 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.

ML 171 Dilution Calculator

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ML 171 Molarity Calculator

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Preparing Stock Solutions of ML 171

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.144 mL 20.7202 mL 41.4405 mL 82.8809 mL 103.6012 mL
5 mM 0.8288 mL 4.144 mL 8.2881 mL 16.5762 mL 20.7202 mL
10 mM 0.4144 mL 2.072 mL 4.144 mL 8.2881 mL 10.3601 mL
50 mM 0.0829 mL 0.4144 mL 0.8288 mL 1.6576 mL 2.072 mL
100 mM 0.0414 mL 0.2072 mL 0.4144 mL 0.8288 mL 1.036 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on ML 171

Combating oxidative stress in vascular disease: NADPH oxidases as therapeutic targets.[Pubmed:21629295]

Nat Rev Drug Discov. 2011 Jun;10(6):453-71.

NADPH oxidases are a family of enzymes that generate reactive oxygen species (ROS). The NOX1 (NADPH oxidase 1) and NOX2 oxidases are the major sources of ROS in the artery wall in conditions such as hypertension, hypercholesterolaemia, diabetes and ageing, and so they are important contributors to the oxidative stress, endothelial dysfunction and vascular inflammation that underlies arterial remodelling and atherogenesis. In this Review, we advance the concept that compared to the use of conventional antioxidants, inhibiting NOX1 and NOX2 oxidases is a superior approach for combating oxidative stress. We briefly describe some common and emerging putative NADPH oxidase inhibitors. In addition, we highlight the crucial role of the NADPH oxidase regulatory subunit, p47phox, in the activity of vascular NOX1 and NOX2 oxidases, and suggest how a better understanding of its specific molecular interactions may enable the development of novel isoform-selective drugs to prevent or treat cardiovascular diseases.

A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells.[Pubmed:20715845]

ACS Chem Biol. 2010 Oct 15;5(10):981-93.

The NADPH oxidase (Nox) proteins catalyze the regulated formation of reactive oxygen species (ROS), which play key roles as signaling molecules in several physiological and pathophysiological processes. ROS generation by the Nox1 member of the Nox family is necessary for the formation of extracellular matrix (ECM)-degrading, actin-rich cellular structures known as invadopodia. Selective inhibition of Nox isoforms can provide reversible, mechanistic insights into these cellular processes in contrast to scavenging or inhibition of ROS production. Currently no specific Nox inhibitors have been described. Here, by high-throughput screening, we identify a subset of phenothiazines, 2-acetylphenothiazine (here referred to as ML171) (and its related 2-(trifluoromethyl)-phenothiazine) as nanomolar, cell-active, and specific Nox1 inhibitors that potently block Nox1-dependent ROS generation, with only marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms. ML171 also blocks the ROS-dependent formation of ECM-degrading invadopodia in colon cancer cells. Such effects can be reversed by overexpression of Nox1 protein, which is suggestive of a selective mechanism of inhibition of Nox1 by this compound. These results elucidate the relevance of Nox1-dependent ROS generation in mechanisms of cancer invasion and define ML171 as a useful Nox1 chemical probe and potential therapeutic agent for inhibition of cancer cell invasion.

Description

ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.

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