136164-66-4
E3330((E)-2-((4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylene)undecanoic acid)
CAS: 136164-66-4
化学式: C21H30O6
| 中文名 | E3330 |
| 英文名 | (E)-2-((4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylene)undecanoic acid |
| 别名 | 化合物E3330 |
| 英文别名 | E3330 E 3330 E-3330 APX3330 CS-1756 APX 3330 (E)-2-((4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylene)undecanoic acid (2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid Undecanoic acid, 2-[(4,5-dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-, (2E)- (2E)-2-[(4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylidene]undecanoic acid E3330 |
| CAS | 136164-66-4 |
| EINECS | 604-604-1 |
| 化学式 | C21H30O6 |
| 分子量 | 378.46 |
| 密度 | 1.13±0.1 g/cm3(Predicted) |
| 熔点 | 56-57 °C |
| 沸点 | 542.2±50.0 °C(Predicted) |
| 溶解度 | DMSO: >20 mg/mL |
| 酸度系数 | 4.29±0.19(Predicted) |
| 存储条件 | 2-8°C |
| 外观 | 粉末 |
| 颜色 | red to orange |
| 靶点 | Ape-1, Ref-1 |
| 体外研究 | 在体外，E3330通过抑制Ape1氧化还原活性，影响成血管细胞发展。 E3330抑制人胰腺癌细胞系PANC1，XPA1，MIAPACA，BxPC3，和PK9的生长。PANC1细胞中，E3330也会促进细胞周期的结束，抑制HIF-1α的DNA结合活性和胰腺癌细胞的迁移。在JHH6细胞中，E3330通过改变APE1亚细胞转运，防止NF-κB的功能活性，并通过阻断氧化还原反应介导的NF-κB活化，减少TNF-α 和FAs积累诱导的IL-6 和IL-8表达。 |
| 体内研究 | 在患有内毒素介导的肝炎的小鼠体内，E3330 (300 mg/kg, p.o.)减弱血浆肿瘤坏死因子活性的提高，并保护小鼠免受肝损伤。在大鼠模型中，E3330 (100 mg/kg, p.o.)也会保护大鼠免受内毒素和半乳糖诱导的肝损伤。 |
| 参考资料 展开查看 | 1: Cesaratto L, Codarin E, Vascotto C, Leonardi A, Kelley MR, Tiribelli C, Tell G. Specific inhibition of the redox activity of ape1/ref-1 by e3330 blocks tnf-α-induced activation of IL-8 production in liver cancer cell lines. PLoS One. 2013 Aug 15;8(8):e70909. doi: 10.1371/journal.pone.0070909. eCollection 2013. PubMed PMID: 23967134; PubMed Central PMCID: PMC3744539. 2: Kelley MR, Luo M, Reed A, Su D, Delaplane S, Borch RF, Nyland RL 2nd, Gross ML, Georgiadis MM. Functional analysis of novel analogues of E3330 that block the redox signaling activity of the multifunctional AP endonuclease/redox signaling enzyme APE1/Ref-1. Antioxid Redox Signal. 2011 Apr 15;14(8):1387-401. doi: 10.1089/ars.2010.3410. Epub 2011 Jan 4. PubMed PMID: 20874257; PubMed Central PMCID: PMC3061197. 3: Zou GM, Karikari C, Kabe Y, Handa H, Anders RA, Maitra A. The Ape-1/Ref-1 redox antagonist E3330 inhibits the growth of tumor endothelium and endothelial progenitor cells: therapeutic implications in tumor angiogenesis. J Cell Physiol. 2009 Apr;219(1):209-18. doi: 10.1002/jcp.21666. PubMed PMID: 19097035. 4: Zou GM, Maitra A. Small-molecule inhibitor of the AP endonuclease 1/REF-1 E3330 inhibits pancreatic cancer cell growth and migration. Mol Cancer Ther. 2008 Jul;7(7):2012-21. doi: 10.1158/1535-7163.MCT-08-0113. PubMed PMID: 18645011; PubMed Central PMCID: PMC3569736. 5: Saitou Y, Shiraki K, Yamanaka T, Miyashita K, Inoue T, Yamanaka Y, Yamaguchi Y, Enokimura N, Yamamoto N, Itou K, Sugimoto K, Nakano T. Augmentat |
136164-66-4 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.642 ml | 13.211 ml | 26.423 ml |
| 5 mM | 0.528 ml | 2.642 ml | 5.285 ml |
| 10 mM | 0.264 ml | 1.321 ml | 2.642 ml |
| 5 mM | 0.053 ml | 0.264 ml | 0.528 ml |
最后更新：2024-01-02 23:10:35
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