2-Acetylphenothiazine (ML171)

Catalog No.S5304 Batch:S530401

Technical Data

Formula	C₁₄H₁₁NOS
Molecular Weight	241.31	CAS No.	6631-94-3
Solubility (25°C)*	In vitro	DMSO	48 mg/mL (198.91 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

2-Acetylphenothiazine (ML171, 2-APT) is a potent and selective inhibitor of NADPH-oxidase with IC50s of 0.25 μM, 5 μM, 3μM, 5 μM and 5.5 μM for NOX1, NOX2, NOX3, NOX4 and xanthine oxidase, respectively.

Targets

NOX1 ^[1] (HEK293)	NOX3 ^[1] (HEK293)	NOX2 ^[1] (HEK293)	NOX4 ^[1] (HEK293)	xanthine oxidase ^[1] (HEK293)
0.25 μM	3 μM	5 μM	5 μM	5.5 μM

In vitro

ML171 is a potent and selective inhibitor of NOX1, with an IC50 of 129–156 nM in cell-based assays. ML171 is not cytotoxic, and is selective among NOX family members NOX2, NOX3, and NOX4, as well as against xanthine oxidase, another cellular source of ROS. In addition, ML171 is highly effective in inhibiting the cellular production of invadopodia in a human colon cancer cell line. It strongly blocks ROS generation in HT29 cells (IC50HT29 = 0.129 μM)^[2]. ML171 does not inhibit mitochondrial ROS production^[3].

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines DLD1 cells Concentrations 10 μM Incubation Time 1 h Method DLD1 cells were plated on glass coverslips and after 24hrs cells were transfected with active SrcYF or empty vector (mock). 48hrs after transfection, cells were treated as indicated for 1hr with 10 μM of ML171, or with DMSO or 10 μM DPI. Afterwards, cells were fixed and stained and visualized by confocal miscroscopy.

Cell Assay:^{^[3]}

Cell lines
DLD1 cells
Concentrations
10 μM
Incubation Time
1 h
Method
DLD1 cells were plated on glass coverslips and after 24hrs cells were transfected with active SrcYF or empty vector (mock). 48hrs after transfection, cells were treated as indicated for 1hr with 10 μM of ML171, or with DMSO or 10 μM DPI. Afterwards, cells were fixed and stained and visualized by confocal miscroscopy.

References

Selleck's 2-Acetylphenothiazine (ML171) has been cited by 6 publications

ROS-mediated thylakoid membrane remodeling and triacylglycerol biosynthesis under nitrogen starvation in the alga Chlorella sorokiniana [ Front Plant Sci, 2024, 15:1418049]	PubMed: 39040507
A predicted structure of NADPH Oxidase 1 identifies key components of ROS generation and strategies for inhibition [ PLoS One, 2023, 18(5):e0285206]	PubMed: 37134122
A Histone Deacetylase Inhibitor Induces Acetyl-CoA Depletion Leading to Lethal Metabolic Stress in RAS-Pathway Activated Cells [ Cancers (Basel), 2022, 14(11)2643]	PubMed: 35681624
G Protein-Coupled Estrogen Receptor Agonist G-1 Inhibits Mantle Cell Lymphoma Growth in Preclinical Models [ Front Oncol, 2021, 11:668617]	PubMed: 34211844
Reactive oxygen species mediate thylakoid membrane remodeling and triacylglycerol synthesis under nitrogen starvation in the algaChlorella sorokiniana [ bioRxiv, 2021, 10.1101/2021.05.15.444036]	PubMed: none
Oxidation of Reduced Graphene Oxide via Cellular Redox Signaling Modulates Actin-Mediated Neurotransmission. [ ACS Nano, 2020, 24;14(3):3059-3074]	PubMed: 32057235

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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