| 产品描述: | UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells |
| 靶点: |
Ki: 0.41 μM (Urokinase-type plasminogen activator (uPA)) Serine protease;Others |
| 体外研究: |
UKI-1 (WX-UK1; 0.1-1.0 μg/mL) treatment shows a decrease of tumor cell invasion by up to 50% is achieved in both models with the SCCHN line FaDu and the cervical carcinoma line HeLa. UKI-1 (WX-UK1) interferes with the plasminogen activation system at 2 levels: it inhibits plasmin formation directly and via inhibition of uPA. In vitro invasion models with highly invasive fibrosarcoma and breast cancer cells showed that UKI-1 effectively inhibits migration of the cells through fibrin matrices |
| 体内研究: |
UKI-1 (WX-UK1) treatment has antimetastatic activities that significantly reduces the number of metastatic lesions and tumor growth in metastasizing rat pancreatic and mammary adenocarcinoma tumor models |
| 参考文献: |
1. Ertongur S et al. Inhibition of the invasion capacity of carcinoma cells by WX-UK1, a novel synthetic inhibitor of the urokinase-type plasminogen activator system. Int J Cancer. 2004 Jul 20;110(6):815-24. 2. Ewa Zeslawska et al. Crystals of the urokinase type plasminogen activator variant βc-uPA in complex with small molecule inhibitors open the way towards structure-based drug design. J Mol Biol. 2000 Aug 11;301(2):465-75. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.629 ml |
8.146 ml |
16.292 ml |
| 5 mM |
0.326 ml |
1.629 ml |
3.258 ml |
| 10 mM |
0.163 ml |
0.815 ml |
1.629 ml |
| 50 mM |
0.033 ml |
0.163 ml |
0.326 ml |
|
| 注意: |
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