An APE1/Ref-1 redox activity inhibitor; inhibits APE1-mediated AP-1 DNA binding activity (IC50 = 6.5 µM in a redox EMSA) but has no effect on APE1 DNA repair activity in endonuclease or gap-filling assays from 0.01-50 µM; reduces activation of NF-κB

E3330 – 10 mg

Brand:
Cayman
CAS:
136164-66-4
Storage:
-20
UN-No:
- /

E3330 is an inhibitor of apurinic-apyrimidinic endonuclease 1/redox factor-1 (APE1/Ref-1) redox activity.{59711,59712} 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.{59711} E3330 reduces basal activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 pancreatic cancer cells.{59712} 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.  

 

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Description

An APE1/Ref-1 redox activity inhibitor; inhibits APE1-mediated AP-1 DNA binding activity (IC50 = 6.5 µM in a redox EMSA) but has no effect on APE1 DNA repair activity in endonuclease or gap-filling assays from 0.01-50 µM; reduces activation of NF-κB, AP-1, and HIF-1 in reporter assays using PANC-1 cells; inhibits proliferation of PaCa-2 and PANC-1 pancreatic cancer cells (EC50s = 135 and 87 µM, respectively); inhibits tumor growth in a PaCa-2 mouse xenograft model and pancreatic cancer PDX mouse models at 25 mg/kg

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

Synonyms:  APX 3330

Molecular weight: 378.5

CAS: 136164-66-4

Purity: ≥98%

Formulation: A solid

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