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

Cat. No.: HY-12805 Purity: 99.50%
Handling Instructions

ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective 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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
500 mg USD 100 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective 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].

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.
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
Molecular Weight

241.31

Formula

C₁₄H₁₁NOS

CAS No.

6631-94-3

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ML171
Cat. No.:
HY-12805
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ML171

Cat. No.: HY-12805