您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > E3330
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
E3330
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
E3330图片
CAS NO:136164-66-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
E3330 (APX-3330) 是 Ape-1(无嘌呤/无嘧啶核酸内切酶 1)/Ref-1(氧化还原因子-1)氧化还原的直接、口服活性和选择性抑制剂。
Cas No.136164-66-4
别名APX-3330
化学名(E)-2-((4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylene)undecanoic acid
Canonical SMILESCCCCCCCCC/C(C(O)=O)=C([H])\C(C1=O)=C(C(C(OC)=C1OC)=O)C
分子式C21H30O6
分子量378.46
溶解度≥ 75.4mg/mL in DMSO, ≥ 75.4mg/mL in EtOH
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

AP endonuclease 1 (APE1) is a dual-function protein, which contains a redox domain and a DNA repair domain. APE1 is overexpressed in numerous solid cancers, including prostate and bladder cancers, non-small cell lung cancers, gliomas, medulloblastomas and primitive neurectodermal tumors, osteosarcomas, and germ cell tumors. E3330 is a small molecule inhibitor of redox activity of APE1 protein.

In vitro: E3330 significantly reduces the growth of human pancreatic cancer cells in vitro. This phenomenon was further confirmed by a small interfering RNA experiment to knockdown APE1 expression in pancreatic cancer cells. Furthermore, the growth-inhibitory effects of E3330 are accentuated by hypoxia, and this is accompanied by striking inhibition in the DNA binding ability of hypoxia-inducible factor-1α [1].

In vivo: Oral pretreatment with E3330 attenuated the elevation of plasma tumor necrosis factor activity and protected micefrom liver injury. Furthermore, E3330 inhibited the production of tumor necrosis factor from cultured Propionibacterium acnes-elicited murine peritoneal macrophages on stimulation with lipopolysaccharide in vitro [2].

Clinical trial: Up to now, E3330 is still in the preclinical development stage.

Reference:
[1] Gang-Ming Zou and Anirban Maitra. 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): 2012–2021.
[2] Nagakawa J, Hishinuma I, Miyamoto K, Hirota K, Abe S, Yamanaka T, Katayama K, Yamatsu I. Protective effects of (2E)-3-[5-(2,3-dimethoxy-6-methyl-1,4- benzoquinoyl)]-2-nonyl-2-propenoic acid on endotoxin-mediated hepatitis in mice. J Pharmacol Exp Ther. 1992 Jul;262(1):145-50.