产品说明
一般描述
This compound is a cell-permeable, selective, and reversible thiopyrimidone MMP-9 allosteric inhibitor that binds specifically to the non-catalytic site of MMP-9 at the PEX domain with a Kd = 2.1 µM and thereby disrupts MMP-9 homodimerization and its cross-talk with CD44 and the EGFR-MAPK signaling pathway. It does not bind to the PEX domain of MMP-2 or MT1-MMP and it is shown to decrease MMP-9 mediated cell migration in COS-1 cells at 100 µM. Also, it inhibits cell migration and invasion of HT-1080 and MDA-MB-435 human cancer cells in a dose-dependent manner from 0.1 to 100 µM, without altering MMP-9 expression or proteolytic activity in HT-1080 cells. In addition, it attenuates both primary tumor growth and metastasis in vivo in a mouse model without obvious toxicity (20 mg/kg, 6 days/week, i.v. and i.t.).
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他说明
Dufour, A., et al. 2011. Cancer Res.71, 4977.
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 | C16H17F2N3O3S |
| 分子量 | 369.39 |
| MDL编号 | MFCD32671875 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | yellow-white |
| 溶解性 | DMSO: 50 mg/mL, light yellow |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(CSC(NC(CCC)=C1)=NC1=O)NC2=CC=C(OC(F)F)C=C2 |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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