UKI-1 (Synonyms: WX-UK1; UKI-1C)
目录号: PL08756 纯度: ≥96%
CAS No. :220355-63-5
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中文名称
UKI-1
中文别名
UKI-1
英文名称
UKI-1
英文别名
UKI-1;UKI 1;UKI 1C;UKI-1C;Wx-uk1 free base;WX-UK1;00LOF6890B;ethyl 4-[(2S)-3-(3-carbamimidoylphenyl)-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate;compound 2r-L;GTPL6498;BDBM23891;Q27089235;1-Piperazinecarboxylic acid, 4-((2S)-3-(3-(aminoiminomethyl)phenyl)-1-oxo-2-(((2,4,6-tris(1-methylethyl)phenyl)sulfonyl)amino)propyl)-, ethyl ester;ethyl 4-[(2S)-3-(3-carbamimid
Cas No.
220355-63-5
分子式
C32H47N5O5S
分子量
613.81
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
UKI-1 (UKI-1C) 是一种有效的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂,Ki 为 0.41 μM。UKI-1 还是一种低分子量的丝氨酸蛋白酶 (serine protease) 抑制剂。UKI-1 是有效的抗转移剂,可抑制癌细胞的侵袭能力。
生物活性
UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a K i 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.
性状
Solid
IC50 & Target[1][2]
Ki: 0.41 μM (Urokinase-type plasminogen activator (uPA))
Serine protease
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (162.92 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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