Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor - NF-κB inhibitor APX-3330 For research use only.

APX-3330

Synonyms: E3330

APX-3330 (E3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

APX-3330 Chemical Structure

APX-3330 Chemical Structure

CAS No. 136164-66-4

Purity & Quality Control

Batch: S744501 DMSO]100 mg/mL]false]Ethanol]75 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

APX-3330 Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hey-C2 cells Function assay Inhibition of Ape1/ref-1 redox activity in presence of 0.02 mM DTT and human Hey-C2 cells nuclear extracts by EMSA, IC50=10μM. 20067291
Hey-C2 cells Growth inhibition assay 72 hrs Growth inhibition of human Hey-C2 cells after 72 hrs by MTS assay, GI50=35μM. 20067291
Click to View More Cell Line Experimental Data

Biological Activity

Description APX-3330 (E3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
Targets
NF-κB [3] APE1(Ref-1) [1]
In vitro
In vitro E3330 affects hemangioblast development in vitro via inhibition of Ape1 redox activity. [1] E3330 inhibits the growth of human pancreatic cancer cell line PANC1, XPA1, MIAPACA, BxPC3, and PK9. E3330 also promotes exit of cell cycle in PANC1 cells, inhibits the DNA-Binding activity of HIF-1α and migration of pancreatic cancer cells. [2] In JHH6 cells, E3330 prevents the functional activation of NF-κB via the alteration of APE1 subcellular trafficking and reduces IL-6 and IL-8 expression induced by TNF-α and FAs accumulation through blockage of the redox-mediated activation of NF-κB. [3]
Cell Research Cell lines PANC1 cells
Concentrations ~30 μM
Incubation Time 72 hours
Method PANC1 cells are placed in one well of a 12-well plate and treated with 5 to 30 μM E3330. After a 24, 48, and 72 h of culture, the cells are washed with PBS and stained with trypan blue, and cell viability is examined by counting the live cell numbers.
In Vivo
In vivo In mice with endotoxin-mediated hepatitis, E3330 (300 mg/kg, p.o.) attenuates the elevation of plasma tumor necrosis factor activity and protectes mice from liver injury. [4] In Rat model, E3330 (100 mg/kg, p.o.) also protectes rats from severe liver injury induced with endotoxin plus galactosamine. [5]
Animal Research Animal Models Mice with endotoxin-mediated hepatitis
Dosages 300 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03375086 Completed
Cancer
Apexian Pharmaceuticals Inc.
 January 30 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 378.46 Formula

C21H30O6
CAS No. 136164-66-4 SDF Download APX-3330 SDF
Smiles CCCCCCCCCC(=CC1=C(C(=O)C(=C(C1=O)OC)OC)C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (264.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 75 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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