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Merck
CN

E8534

E3330

≥98% (HPLC)

别名:

(2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid

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关于此项目

经验公式(希尔记法):
C21H30O6
化学文摘社编号:
分子量:
378.46
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平

方案

≥98% (HPLC)

表单

powder

颜色

red to orange

溶解性

DMSO: >20 mg/mL

储存温度

2-8°C

SMILES字符串

CCCCCCCCC\C(=C/C1=C(C)C(=O)C(OC)=C(OC)C1=O)C(O)=O

InChI

1S/C21H30O6/c1-5-6-7-8-9-10-11-12-15(21(24)25)13-16-14(2)17(22)19(26-3)20(27-4)18(16)23/h13H,5-12H2,1-4H3,(H,24,25)/b15-13+

InChI key

AALSSIXXBDPENJ-FYWRMAATSA-N

应用

E3330 has been used in the inhibition of endothelial cancer cells and apurinic/apyrimidinic endodeoxyribonuclease 1 (APEX1).

生化/生理作用

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.
E3330 is a specific inhibitor of AP endonuclease 1 redox domain; inhibits APE-1 regulation of transcription factors, but does not affect Ape1 DNA repair activity.

危险声明

预防措施声明

危险分类

Aquatic Chronic 4

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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Brittney A Manvilla et al.
Biochemistry, 50(48), 10540-10549 (2011-10-29)
AP endonuclease 1 (APE1) is a multifaceted protein with essential roles in DNA repair and transcriptional regulation. APE1 (ref-1) activates many transcription factors (TF), including AP-1 and NF-κB. While the mechanism of APE1 redox activity remains unknown, it may involve
Mark R Kelley et al.
Antioxidants & redox signaling, 14(8), 1387-1401 (2010-09-30)
APE1 is a multifunctional protein possessing DNA repair and redox activation of transcription factors. Blocking these functions leads to apoptosis, antiangiogenesis, cell-growth inhibition, and other effects, depending on which function is blocked. Because a selective inhibitor of the APE redox
[Elucidation of pharmacological mechanism of drugs by studying the receptors].
Hiroshi Handa
The Japanese journal of antibiotics, 56 Suppl A, 39-46 (2003-12-19)
N Shimizu et al.
Nature biotechnology, 18(8), 877-881 (2000-08-10)
We have developed a method using novel latex beads for rapid identification of drug receptors using affinity purification. Composed of a glycidylmethacrylate (GMA) and styrene copolymer core with a GMA polymer surface, the beads minimize nonspecific protein binding and maximize
Barbara Frossi et al.
The Journal of biological chemistry, 294(13), 5198-5207 (2019-02-02)
The base excision repair (BER) pathway is an important DNA repair pathway and is essential for immune responses. In fact, it regulates both the antigen-stimulated somatic hypermutation (SHM) process and plays a central function in the process of class switch

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