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Dicoumarol

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Chemical Structure| 66-76-2 同义名 : 双羟香豆素 ;Dicumarol;NSC 17860;Antitrombosin;Melitoxin;Dicoumarin;Bishydroxycoumarin;NSC 221570;NSC 41834
CAS号 : 66-76-2
货号 : A205533
分子式 : C19H12O6
纯度 : 95%
分子量 : 336.295
MDL号 : MFCD00006857
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 3 mg/mL(8.92 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(74.34 mM)，配合低频超声，并调节pH至11
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
描述 Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively[3]. DIC (Dicoumarol) potently inhibited the kinase activity of PDK1(Pyruvate dehydrogenase kinase 1), shifted the glucose metabolism from aerobic glycolysis to oxidative phosphorylation, generated a higher level of reactive oxygen species (ROS), attenuated the mitochondrial membrane potential (MMP), induced apoptosis, and reduced cell viability in vitro[4]. Exposure of erythrocytes for 48 hours to dicoumarol (=10 μM) significantly increased [Ca(2+)](i), enhanced cation channel activity, decreased forward scatter, triggered annexin-V-binding and elicited hemolysis. Dicoumarol stimulates suicidal death of erythrocytes by stimulating Ca(2+) entry and subsequent triggering of Ca(2+) dependent cell membrane scrambling[5]. Moreover, dicoumarol synergized with emodin to sensitize HeLa cells to As2O3(arsenic trioxide)-induced apoptosis through raising the ROS (reactive oxygen species) level[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.87mL

2.97mL

1.49mL

29.74mL

5.95mL

2.97mL
参考文献

[1]Bian J, Li X, et al. Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Feb 15;127:828-839.

[2]Zhang W, Su J, et al. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672.

[3]Bian J, Li X, Xu L, Wang N, Qian X, You Q, Zhang X. Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Feb 15;127:828-839

[4]Zhang W, Su J, Xu H, Yu S, Liu Y, Zhang Y, Sun L, Yue Y, Zhou X. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672

[5]Qadri SM, Kucherenko Y, Zelenak C, Jilani K, Lang E, Lang F. Dicoumarol activates Ca2+-permeable cation channels triggering erythrocyte cell membrane scrambling. Cell Physiol Biochem. 2011;28(5):857-64

[6]Jing YW, Yi J, Chen YY, Hu QS, Shi GY, Li H, Tang XM. Dicoumarol alters cellular redox state and inhibits nuclear factor kappa B to enhance arsenic trioxide-induced apoptosis. Acta Biochim Biophys Sin (Shanghai). 2004 Mar;36(3):235-42