APE1 Redox Inhibitor

E3330 Chemical Information:
Synonym: (2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid
Molecular Weight: 378.459
Empirical Formula: C21H30O6
CAS Number: 136164-66-4
HPLC purity is >= to 97%
Solubility: DMSO: >20 mg/mL
Form: powder
Color: orange

E3330 represents a novel class of inhibitor. Unlike other compounds that target APE1, it has been recently reported that E3330 recognizes an alternate, redox active conformation of APE1, and that it potentially inhibits APE1's redox activity by inducing disulfide bond formation. No other compound has been reported to selectively recognize an alternate conformation of APE1 or work through this type of mechanism. Thus, E3330 represents a novel class of inhibitor. E3330 was originally developed as an NFkB inhibitor, but subsequently APE1 was found to bind to E3330 through affinity pull-down experiments using immobilized E3330. In light of later work demonstrating that APE1 regulates the transcriptional activity of NFkB, we now know that E3330 actually works upstream of NFkB by inhibiting APE1. Although many quinone compounds have undesirable properties including susceptibility to Michael additions by nucleophiles, E3330 does not form covalent adducts with APE1 because there is no substituent that can serve as an effective leaving group.

This product is for research use only and is not approved for use in humans or in clinical diagnosis. Inhibitors are guaranteed for 1 year from date of receipt.

Showing Publications 1 - 10 of 12. Show All 12 Publications. Collapse Publications.

Publications using NBP1-49581	Applications	Species
Lu H, Bhat AA, Peng D et al. APE1 upregulates MMP-14 via redox-sensitive ARF6-mediated recycling to promote cell invasion of esophageal adenocarcinoma Cancer Res. 2019-07-15 [PMID: 31308045]
Cesaratto L, Codarin E, Vascotto C et al. Specific inhibition of the redox activity of ape1/ref-1 by e3330 blocks tnf-a-induced activation of IL-8 production in liver cancer cell lines. PLoS One 2013-08-15 [PMID: 23967134]
Zhang J, Luo M, Marasco D et al. Inhibition of apurinic/apyrimidinic endonuclease I's redox activity revisited. Biochemistry. 2013-04-30 [PMID: 23597102]
Cardoso AA, Jiang Y, Luo M et al. APE1/Ref-1 regulates STAT3 transcriptional activity and APE1/Ref-1-STAT3 dual-targeting effectively inhibits pancreatic cancer cell survival. PLoS One 2012-01-01 [PMID: 23094050]
Luo M, Zhang J, He H et al. Characterization of the redox activity and disulfide bond formation in apurinic/apyrimidinic endonuclease. Biochemistry. 2012-01-17 [PMID: 22148505]
Vasko MR, Guo C, Thompson EL, Kelley MR. The repair function of the multifunctional DNA repair/redox protein APE1 is neuroprotective after ionizing radiation. DNA Repair (Amst). 2011-09-05 [PMID: 21741887]
Fishel ML, Jiang Y, Rajeshkumar NV et al. Impact of APE1/Ref-1 redox inhibition on pancreatic tumor growth. Mol Cancer Ther. 2011-09-01 [PMID: 21700832]
Jedinak A, Dudhgaonkar S, Kelley MR, Sliva D. Apurinic/Apyrimidinic endonuclease 1 regulates inflammatory response in macrophages. Anticancer Res 2011-02-01 [PMID: 21378315]
Su D, Delaplane S, Luo M, Rempel DL, Vu B, Kelley MR, Gross ML, Georgiadis MM. Interactions of Apurinic/Apyrimidinic Endonuclease with a Redox Inhibitor: Evidence for an Alternate Conformation of the Enzyme. Biochemistry. 2010-12-08 [PMID: 21117647]
Jiang A, Gao H, Kelley MR, Qiao X. Inhibition of APE1/Ref-1 redox activity with APX3330 blocks retinal angiogenesis in vitro and in vivo. Vision Res 2011-01-01 [PMID: 20937296]
Hiramoto M, Shimizu N, Nishi T, Shima D, Aizawa S, Tanaka H, Hatakeyama M, Kawaguchi H, Handa H. High-performance affinity beads for identifying anti-NF-kappa B drug receptors. Methods Enzymol;353:81-8. 2002-01-01 [PMID: 12078530]
Show All 12 Publications. Collapse Publications.

Array NBP1-49581

• APE1 Redox Inhibitor