Home Immunology & Inflammation NADPH-oxidase inhibitor 2-Acetylphenothiazine (ML171)

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2-Acetylphenothiazine (ML171) NADPH-oxidase inhibitor

Cat.No.S5304

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.
2-Acetylphenothiazine (ML171) NADPH-oxidase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 241.31

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Quality Control

Batch: S530401 DMSO]48 mg/mL]false]]]false]]]false Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (198.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 241.31 Formula

C14H11NOS

 Storage (From the date of receipt)
CAS No. 6631-94-3 -- Storage of Stock Solutions

Synonyms 2-APT Smiles CC(=O)C1=CC2=C(C=C1)SC3=CC=CC=C3N2

Mechanism of Action

Targets/IC50/Ki
NOX1
(HEK293)
0.25 μM
NOX3
(HEK293)
3 μM
NOX2
(HEK293)
5 μM
NOX4
(HEK293)
5 μM
xanthine oxidase
(HEK293)
5.5 μM
In vitro
2-Acetylphenothiazine (ML171) is a potent and selective inhibitor of NOX1, with an IC50 of 129–156 nM in cell-based assays. It 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, this compound 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). ML171 does not inhibit mitochondrial ROS production.
References

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