产品说明
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
10 mg in Glass bottle
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
基本信息
| 经验(实验)分子式 | C14H11NOS |
| 分子量 | 241.31 |
| MDL编号 | MFCD00005017 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | 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℃ |
| 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 |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
