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492002

Sigma-Aldrich

NOX1 Inhibitor, ML171

The NOX1 Inhibitor, ML171, also referenced under CAS 6631-94-3, controls the biological activity of NOX1.

同義詞:

NOX1 Inhibitor, ML171, NADPH Oxidase-1 Inhibitor, ML171, 2-APT, 2-acetylphenothiazine

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About This Item

經驗公式(希爾表示法):
C14H11NOS
CAS號碼:
分子量::
241.31
MDL號碼:
分類程式碼代碼:
41121801
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

powder

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

dark yellow-orange

溶解度

DMSO: 50 mg/mL

運輸包裝

ambient

儲存溫度

2-8°C

InChI

1S/C14H11NOS/c1-9(16)10-6-7-14-12(8-10)15-11-4-2-3-5-13(11)17-14/h2-8,15H,1H3

InChI 密鑰

JWGBOHJGWOPYCL-UHFFFAOYSA-N

一般說明

A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC50 = 0.129 µM, and 0.25 µM) in human HT29 and HEK293 cell-based assays, respectively. Unlike most other currently used Nox inhibitors, it only has marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms (IC50 = 5 µM, 3 µM and 5 µM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC50 = 5.5 µM) in HEK293 cell-based assays. It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ~ 100 nM; however, its inhibitory effect is reversed through over-expression of Nox1, thereby suggesting that this compound is highly selective for Nox1, with little effect against Nox2-dependent ROS generation (IC50 >10 µM). Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.
A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC50 = 0.129 µM, and 0.25 µM) in human HT29 and HEK293 cell-based assays, respectively. Unlike most other currently used Nox inhibitors, it only has marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms (IC50 = 5 µM, 3 µM and 5 µM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC50 = 5.5 µM) in HEK293 cell-based assays. It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ~100 nM; however, its inhibitory effect is reversed through over-expression of Nox1, thereby suggesting that this compound is highly selective for Nox1, with little effect against Nox2-dependent ROS generation (IC50 >10 µM). Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.

包裝

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Gianni, D., et al. 2010. ACS Chem. Biol.5, 981.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


分析證明 (COA)

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Tamara Seredenina et al.
Free radical biology & medicine, 86, 239-249 (2015-05-28)
NADPH oxidases (NOXs) constitute a family of enzymes generating reactive oxygen species (ROS) and are increasingly recognized as interesting drug targets. Here we investigated the effects of 10 phenothiazine compounds on NOX activity using an extensive panel of assays to
Jing Sun et al.
Frontiers in pharmacology, 12, 751845-751845 (2021-10-16)
Receptor activator of nuclear factor-κB ligand (RANKL) has been found to induce osteoclastogenesis and bone resorption. However, the underlying molecular mechanisms remain unclear. Via conducting a series of biochemical experiments with in vitro cell lines, this study investigated the role
Sori Kim et al.
Molecular medicine reports, 24(6) (2021-10-06)
Astaxanthin (ASX), a red‑colored xanthophyll carotenoid, functions as an antioxidant or pro‑oxidant. ASX displays anticancer effects by reducing or increasing oxidative stress. Reactive oxygen species (ROS) promote cancer cell death by necroptosis mediated by receptor‑interacting protein kinase 1 (RIP1) and RIP3. NADPH

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