推荐产品
质量水平
方案
≥95% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
dark yellow-orange
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
S1c2c(cc(cc2)C(=O)C)Nc3c1cccc3
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 key
JWGBOHJGWOPYCL-UHFFFAOYSA-N
一般描述
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.
包装
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Gianni, D., et al. 2010. ACS Chem. Biol.5, 981.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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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