2. Metabolic Enzyme/Protease
  3. NADPH Oxidase
  4. ML171

ML171  (Synonyms: 2-Acetylphenothiazine; 2-APT)

Cat. No.: HY-12805 Purity: 99.82%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

ML171 Chemical Structure

ML171 Chemical Structure

CAS No. : 6631-94-3

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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
100 mg USD 50 In-stock
500 mg USD 100 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ML171 purchased from MCE. Usage Cited in: Inflammation. 2023 Feb 20.  [Abstract]

    In rat NP cells, ML171 inhibits the expression of catabolic markers MMP13, ADAMTS4, ADAMTS5, and pyroptotic markers NLRP3, GSDMD-NT, and cleaved-caspase-1, as well as incresaes the expression of ECM anabolic markers COL2A and ACAN, by inhibiting overexpression of BRD9 (Fig. c and d).

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    • References

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    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.

    IC50 & Target

    IC50: 0.25 μM (HEK293-Nox1), 0.129 μM (HT29)[1]
    In Vitro

    Nox1-dependent ROS generation has been shown to play a pivotal role in cell signaling, cell growth, angiogenesis, motility and blood pressure regulation. ML171 strongly blocks ROS generation in HT29 cells (IC50=0.129 μM) and only increasing over-expression of Nox1 can overcome the blockage of ROS generation caused by ML171 treatment in HEK293 cell system reconstituted with all the components required Nox1-dependent ROS generation. ML171 efficiently blocks ROS production measured by carboxy-H2-DCFDA staining as well as DPI used as a positive control. When ML171 is tested in HEK293-Nox1 reconstituted cell system, higher potency in blocking Nox1-dependent ROS generation is observed compared with the parental compound[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    241.31

    Appearance

    Solid

    Formula

    C14H11NOS
    CAS No.
    SMILES

    CC(C1=CC=C2SC3=CC=CC=C3NC2=C1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 64 mg/mL (265.22 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.1440 mL 20.7202 mL 41.4405 mL
    5 mM 0.8288 mL 4.1440 mL 8.2881 mL
    10 mM 0.4144 mL 2.0720 mL 4.1440 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (10.36 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
    Cell Assay
    [1]

    HT29 cells are cultured in 150 mm diameter plate and when 70-80% confluence is reached, cells are trypsinized, harvested in HBSS and counted. 4×104 cells are dispensed into individual wells in 30 μL final volume (384 well plates) by using a robotic liquid handler. Cells are treated for 60 min at 37°C with 50 nL of DPI, DMSO and library compounds (including ML171) which are automatically dispensed into individual wells from their respective assay plates. This will correspond to a final concentration of 10 μM DPI or library compounds (ML171), and 0.1% DMSO. 20 μL of a mixture containing 200 μM luminol plus 0.32 units of HRP (final concentration) is added. Luminescence is quantified using a 384-well plate luminometer. The data output consisting of the emission intensities for each well is imported into a spread-sheet program (such as Excel) for further processing. As designed, compounds that inhibit Nox1 activity will reduce cellular ROS production, leading to reduced probe-ROS interactions and reduced well luminescence. Compounds are considered ‘hits’ and further processed when light emission is blocked >75% 7 than DMSO wells (DMSO and DPI wells are set to 0% and 100% respectively). Compounds are tested in singlicate at a concentration of 10 μM[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    ML1716631-94-32-Acetylphenothiazine 2-APTML 171ML-171NADPH OxidaseNOXInhibitorinhibitorinhibit

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