Dicoumarol 双香豆素;Dicumarol;NADH:quinone oxidoreductase (NQO1) NADH:醌氧化还原酶;anti-coagulant properties 抗凝特性;Antimycin A抗霉素A;CCCP 解偶联剂;CAS NO:66-76-2;
产品信息
产品名称 | CAS NO. | 规格 |
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Dicoumarol 双香豆素 | 66-76-2 | 1g |
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Dicoumarol 双香豆素 | 66-76-2 | 5g |
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Dicoumarol 双香豆素 | 66-76-2 | 25g |
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双香豆素(Dicoumarol)是一种NADH:醌氧化还原酶(NQO1)的竞争性抑制剂,在不含和含BSA的情况下,IC50分别是2.6和404nM[1]。具有抗增殖活性,靶向胰腺癌细胞MIA PaCa-2和人结肠癌细胞HCT116的IC50分别是52和19μM。人HEK293细胞中双香豆素抑制MEKK1上游和TNF受体关联因子2(TRAF2)下游某点的应激活化蛋白激酶(SAPK)(IC50=33μM)[2]。通过抑制JNK活化也呈现出FL5.12淋巴细胞和MCF-2乳腺癌细胞的抗增殖活性[3]。双香豆素以剂量依赖性的方式抑制PDK1活性,IC50是19.42μM[4]。双香豆素通过干扰维生素K循环,广泛用作一种抗凝剂[5]。
产品特性
化学名:3,3′-methylenebis[4-hydroxy-2H-1-benzopyran-2-one | |
同义名:Dicumarol; 3,3′-Methylenebis(4-hydroxycoumarin); Bishydroxycoumarin; NSC 17860; NSC 41834; NSC 221570; 3,3′-亚甲基双(4-羟基香豆素);双(羟)香豆素; | |
CAS NO:66-76-2 | 分子式:C19H12O6 |
分子量:336.3g/mol |
含量:≥98% |
外观:白色至类白色粉末 |
溶解性:溶于DMSO(2mg/ml) |
保存与运输方法
保存:-20ºC干燥保存,至少2年有效。
运输:室温运输。
注意事项
1) 本品不是临床药物,只能用于科研用途,不能用于诊断或临床用途。
2)为了您的安全和健康,请穿实验服并戴一次性手套操作。
配制储存液
质量
溶剂体积 浓度 |
1mg | 5mg | 10mg | 50mg |
1mM | 2.9736 mL | 14.8681mL | 29.7362mL | 148.6812 mL |
5mM | 0.5947 mL | 2.9736mL | 5.9472 mL | 29.7362 mL |
10mM | 0.2974mL | 1.4868mL | 2.9736mL | 14.8681 mL |
50mM | 0.0595mL | 0.2974mL | 0.5947mL | 2.9736 mL |
参考文献
[1] Nolan KA et al. Synthesis and biological evaluation of coumarin-based inhibitors of NAD(P)H: Quinone oxidoreductase-1 (NQO1). J Med Chem. 2009 Nov 26;52(22):7142-56.
[2] Cross JV et al. Quinone reductase inhibitors block SAPK/JNK and NFκB pathways and potentiate apoptosis. J Biol Chem. 1999 Oct 29;274(44):31150-4.
[3] Krause D et al. Transient activation of Jun N-terminal kinases and protection from apoptosis by the insulin-like growth factor I receptor can be suppressed by dicumarol. J Biol Chem. 2001 Jun 1;276(22):19244-52.
[4] Zhang W et al. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672.
[5] Tsoucalas G, et al. Historical Hallmarks of Anticoagulation and Antiplatelet Agents. Curr Pharm Des. 2016; 22: 1857–1861.
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