• 生物活性

靶点及简介 ：Ape-1/Ref-1 inhibitor

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 is a specific inhibitor of AP endonuclease 1 redox domain. E3330 inhibits APE-1 regulation of transcription factors, but does not affect Ape1 DNA repair activity. AP endonuclease 1 (APE1; also known as REF-1) is a multifunctional protein with dual functions in DNA repair and redox regulation of transcription factors. It is involved in apurinic/apyrimidinic endonuclease DNA base excision repair activity, in proofreading exonuclease activity, and in modulating DNA binding activity of several transcription factors including NF-κB, Egr-1, p53, AP-1, CREB, HIF-α, and members of the Pax family. APE1 is overexpressed in several human cancers, and disruption of APE1 function has detrimental effects on cancer cell viability. E3330 significantly reduces the growth of human pancreatic cancer cells in vitro and inhibits pancreatic cancer cell migration.

• 验证及参考文献

验证：

参考文献：

• [1] Zou GM, et al. Blood. 2007, 109(5), 1917-1922.
• [2] Zou GM, et al. Mol Cancer Ther. 2008, 7(7), 2012-2021.
• [3] Cesaratto L, et al. PLoS One. 2013, 8(8), e70909.

• [4] Nagakawa J, et al. J Pharmacol Exp Ther. 1992, 262(1), 145-150.
• [5] Nagakawa J, et al. J Pharmacol Exp Ther. 1993, 264(

• 溶解度及制备方案
  

  DMSO	100 mg/mL  (264.23 mM)
  Ethanol	75 mg/mL  (198.17 mM)
  Water	Insoluble

制备储备液

浓度   溶剂体积    质量	1 mg	5 mg	10 mg
1 mM	2.6423 mL	13.2114 mL	26.4229 mL
5 mM	0.5285 mL	2.6423 mL	5.2846 mL
10 mM	0.2642 mL	1.3211 mL	2.6423 mL
50 mM	0.0528 mL	0.2642 mL	0.5285 mL

• 
  关键词：E3330, E3330供应商, 购买E3330, E3330溶解度, E3330结构式