APE1 Redox Inhibitor

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APE1 Redox Inhibitor [NBP1-49581] - Chemical Structure of E3330 [NBP1-49581]

Product Details

Summary
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E3330

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APE1 Redox Inhibitor Summary

Specificity
E3330 is a chemical that inhibits the redox activity of APE1.

Applications/Dilutions

Application Notes
E3330 is useful for inhibiting APE1 redox activity.
Publications
Read Publications using NBP1-49581.

Packaging, Storage & Formulations

Storage
Store at -20C in powder form. Store at -80C once reconstituted.
Buffer
This product is supplied as a powder. It is soluble in DMSO (>20 mg/mL).

Notes

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

Please go the "Publications, Images, Reviews & Protocols" tab and look under "General Protocols" for this product's MSDS.

Alternate Names for APE1 Redox Inhibitor

  • (2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid
  • 3330
  • AP endonuclease 1 Inhibitor
  • APE-1 Inhibitor
  • APEX 1 Inhibitor
  • Apurinic Endonuclase Factor 1 Inhibitor
  • APX3330
  • E-3330
  • REF1 Inhibitor
  • REF-1 Inhibitor

Background

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.

Limitations

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.

Publications for APE1 Redox Inhibitor (NBP1-49581)(10)


Showing Publications 1 - 10 of 10.
Publications using NBP1-49581 Applications Species
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 Aug 15 [PMID: 23967134]
Zhang J, Luo M, Marasco D et al. Inhibition of apurinic/apyrimidinic endonuclease I's redox activity revisited. Biochemistry. 2013 Apr 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 [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 Jan 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 Sep 5 [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 Sep [PMID: 21700832]
Jedinak A, Dudhgaonkar S, Kelley MR, Sliva D. Apurinic/Apyrimidinic endonuclease 1 regulates inflammatory response in macrophages. Anticancer Res 2011 Feb [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 Dec 8. [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 Jan [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 [PMID: 12078530]

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Product General Protocols

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