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  • Product Name: ML 171
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6631-94-3

6631-94-3 structure
6631-94-3 structure
  • Name: ML171
  • Chemical Name: 2-Acetylphenothiazine
  • CAS Number: 6631-94-3
  • Molecular Formula: C14H11NOS
  • Molecular Weight: 241.30800
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2018-04-12 08:00:00
  • Modify Date: 2024-01-01 23:09:51
  • 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.
Name 2-Acetylphenothiazine
Synonyms 2-acetyl-1-phenothiazine
EINECS 229-626-4
2-Acetyl-10H-phenothiazine
1-phenothiazin-2-yl-ethanone
2-acetyl-phenothiazine
MFCD00005017
1-(10H-phenothiazin-2-yl)ethanone
methyl phenothiazin-2-yl ketone
ML171
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.
Related Catalog
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].
Cell Assay 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].
References

[1]. Gianni D, et al. A novel and specific NADPH oxidase-1 (Nox1) small-molecule inhibitor blocks the formation of functional invadopodia in human colon cancer cells. ACS Chem Biol. 2010 Oct 15;5(10):981-93.

Density 1.249 g/cm3
Boiling Point 455.7ºC at 760 mmHg
Melting Point 180-185 °C(lit.)
Molecular Formula C14H11NOS
Molecular Weight 241.30800
Flash Point 229.4ºC
Exact Mass 241.05600
PSA 54.40000
LogP 4.23540
Index of Refraction 1.653
Hazard Codes Xn
Risk Phrases 22-52/53
Safety Phrases 60-61
WGK Germany 3
HS Code 2934300000
HS Code 2934300000
Summary 2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Chemsrc provides CAS#:6631-94-3 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 6631-94-3 | Chemsrc address: https://www.chemsrc.com/en/baike/667866.html

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