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Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
Table 3Selectivity of parent hit and probe compounds compared to that of chlorpromazine
| Compound | Structure | IC50 (μM) HT29 (NOX1) | IC50 (μM) HEK293-NOX1 | IC50 (μM) HEK293-NOX2 | IC50 (μM) HEK293-NOX3 | IC50 (μM) HEK293-NOX4 | IC50 (μM) Xanthine oxidase |
|---|---|---|---|---|---|---|---|
| 2-(trifluoromethyl)-phenothiazine (parent hit; compound 3) |
 | 0.32 | 1.00 | 9.00 | 7.50 | 5.00 | 5.00 |
| 2-acetylphenothiazine (probe, compound 1) |
 | 0.129 | 0.25 | 5.00 | 3.00 | 5.00 | 5.50 |
| Chlorpromazine (negative control) |
 | >50 | ND | ND | ND | ND | ND |
| DPI (positive control) | 0.2 | 1.2 | 0.5 | 0.75 | 1.1 | 0.005 |
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- Identification and Characterization of a Novel NADPH Oxidase 1 (Nox1) Inhibitor That Suppresses Proliferation of Colon and Stomach Cancer Cells.[Biol Pharm Bull. 2018]Identification and Characterization of a Novel NADPH Oxidase 1 (Nox1) Inhibitor That Suppresses Proliferation of Colon and Stomach Cancer Cells.Yamamoto T, Nakano H, Shiomi K, Wanibuchi K, Masui H, Takahashi T, Urano Y, Kamata T. Biol Pharm Bull. 2018 Mar 1; 41(3):419-426. Epub 2017 Dec 22.
- A subset of N-substituted phenothiazines inhibits NADPH oxidases.[Free Radic Biol Med. 2015]A subset of N-substituted phenothiazines inhibits NADPH oxidases.Seredenina T, Chiriano G, Filippova A, Nayernia Z, Mahiout Z, Fioraso-Cartier L, Plastre O, Scapozza L, Krause KH, Jaquet V. Free Radic Biol Med. 2015 Sep; 86:239-49. Epub 2015 May 23.
- Review Probe Report for NOX1 Inhibitors.[Probe Reports from the NIH Mol...]Review Probe Report for NOX1 Inhibitors.Brown SJ, Gianni D, Bokoch G, Mercer BA, Hodder P, Rosen HR. Probe Reports from the NIH Molecular Libraries Program. 2010
- Review The NOX family of ROS-generating NADPH oxidases: physiology and pathophysiology.[Physiol Rev. 2007]Review The NOX family of ROS-generating NADPH oxidases: physiology and pathophysiology.Bedard K, Krause KH. Physiol Rev. 2007 Jan; 87(1):245-313.
- Table 3, Selectivity of parent hit and probe compounds compared to that of chlor...Table 3, Selectivity of parent hit and probe compounds compared to that of chlorpromazine - Probe Reports from the NIH Molecular Libraries Program
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