E3330

E3330用途

E3330 (APX-3330) 是一种直接,口服有效的 AP 内切核酸酶 1 (APE1; REF-1) 抑制剂,可抑制 NF-κB DNA 结合活性。E3330 (APX-3330) 阻断 TNF-α 诱导的肝癌细胞系中 IL-8 产生的激活。E3330 (APX-3330) 显示出多功能水平的抗癌特性,例如抑制癌细胞的生长和迁移。

E3330名称

[ CAS 号 ]:
136164-66-4

[ 英文名 ]:
E3330

[英文别名 ]:

E3330

E3330生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

[ 靶点 ]

DNA Synthesis, APE1[1-4]

[参考文献]

[1]. Guerreiro PS, et al. The APE1 redox inhibitor E3330 reduces collective cell migration of human breast cancer cells and decreases chemoinvasion and colony formation when combined with docetaxel. Chem Biol Drug Des. 2017 Oct;90(4):561-571.

[2]. Cesaratto L, et al. 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.

[3]. Hiramoto M, et al. Nuclear targeted suppression of NF-kappa B activity by the novel quinone derivative E3330. J Immunol. 1998 Jan 15;160(2):810-9.

[4]. Zou GM, et al. 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.

E3330物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
542.2±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₁H₃₀O₆

[ 分子量 ]:
378.459

[ 闪点 ]:
183.2±23.6 °C

[ 精确质量 ]:
378.204254

[ PSA ]:
89.90000

[ LogP ]:
4.50

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.517

[ 储存条件 ]:
-20℃

E3330MSDS

详细MSDS(安全技术说明书)

E3330安全信息

[ 危害声明 ]:
H413

[ 危险品运输编码 ]:
NONH for all modes of transport

E3330文献

Human apurinic/apyrimidinic endonuclease 1 (APE1) has 3' RNA phosphatase and 3' exoribonuclease activities.

J. Mol. Biol. 427(2) , 298-311, (2015)

Apurinic/apyrimidinic endonuclease 1 (APE1) is the predominant mammalian enzyme in DNA base excision repair pathway that cleaves the DNA backbone immediately 5' to abasic sites. In addition to its aba...

APE1/Ref-1 prevents oxidative inactivation of ERK for G1-to-S progression following lead acetate exposure.

Toxicology 305 , 120-9, (2013)

Apurinic/apyrimidinic endonuclease 1 (APE1)/redox effector factor-1 is a multifunctional enzyme involved in DNA base excision repair and protein redox regulation. Previously, we have showed that lead ...

APE1/Ref-1 regulates STAT3 transcriptional activity and APE1/Ref-1-STAT3 dual-targeting effectively inhibits pancreatic cancer cell survival.

PLoS ONE 7(10) , e47462, (2012)

Pancreatic cancer is a largely incurable disease, and increasing evidence supports strategies targeting multiple molecular mediators of critical functions of pancreatic ductal adenocarcinoma cells. In...

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