An APE1/Ref-1 redox inhibitor
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E3330

Item No. 32830

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-2-[(4,5-dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid
CAS Number
136164-66-4
Synonyms
  • APX-3330
Molecular Formula
C21H30O6
Formula Weight
378.5
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CCCCCCCCC/C(C(O)=O)=C\C(C(C(OC)=C1OC)=O)=C(C)C1=OCCCCCCCCC/C(C(O)=O)=C\C(C(C(OC)=C1OC)=O)=C(C)C1=O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $134

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    10 mg

    $240

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    25 mg

    $565

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    Cayman Chemical
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    Product Description

    E3330 is an inhibitor of apurinic-apyrimidinic endonuclease 1/redox factor-1 (APE1/Ref-1) redox activity.1,2 It inhibits APE1-mediated AP-1 DNA binding activity with an IC50 value of 6.5 µM in a redox EMSA but has no effect on APE1-mediated DNA repair activity in endonuclease or gap-filling assays when used at concentrations ranging from 0.01 to 50 µM.1 E3330 reduces basal activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 pancreatic cancer cells.2 It inhibits proliferation of PaCa-2 and PANC-1 pancreatic cancer cells (EC50s = 135 and 87 µM, respectively). E3330 (25 mg/kg) inhibits tumor growth in a PaCa-2 mouse xenograft model and pancreatic cancer patient-derived xenograft (PDX) mouse models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Luo, M., Delaplane, S., Jiang, A., et al. Role of the multifunctional DNA repair and redox signaling protein Ape1/Ref-1 in cancer and endothelial cells: Small-molecule inhibition of the redox function of Ape1. Antioxid. Redox Signal. 10(11), 1853-1867 (2008).

    2. Fishel, M.L., Jiang, Y., Rajeshkumar, N.V., et al. Impact of APE1/Ref-1 redox inhibition on pancreatic tumor growth. Mol. Cancer Ther. 10(9), 1698-1708 (2011).