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ML171 is a potent and selective inhibitor of NOX1, with an IC50 of 129–156 nM in cell-based assays. 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. 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. 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.
| Cell Experiment | |
|---|---|
| Cell lines | DLD1 cells |
| Preparation 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. |
| Concentrations | 10 μM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 241.31 |
| Formula | C14H11NOS |
| CAS Number | 6631-94-3 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NADPH Oxidase Products |
|---|
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| Apocynin
Apocynin is a nADPH-oxidase inhibitor. |
| VAS2870
VAS2870 is a cell-permeable and specific NADPH oxidase (NOX) inhibitor that effectively suppresses growth factor-mediated ROS liberation in VSMC. |
| APX-115
APX-115 is a potent, orally active inhibitor of pan NADPH oxidase (Nox) with Ki of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. |
| GLX351322
GLX351322 is an NADPH oxidase 4 inhibitor, which inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 uM. |
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