APX-3330

Catalog No.S7445 Batch:S744501

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Technical Data

Formula

C21H30O6
Molecular Weight 378.46 CAS No. 136164-66-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (264.22 mM)
Ethanol 75 mg/mL (198.17 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
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]

Protocol (from reference)

Cell Assay:[2]
  • 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.
Animal Study:[4]
  • Animal Models

    Mice with endotoxin-mediated hepatitis

  • Dosages

    300 mg/kg

  • Administration

    p.o.

Selleck's APX-3330 has been cited by 3 publications

APE1 promotes non-homologous end joining by initiating DNA double-strand break formation and decreasing ubiquitination of artemis following oxidative genotoxic stress [ J Transl Med, 2023, 21(1):183] PubMed: 36894994
Pharmacological inhibition of Ref-1 enhances the therapeutic sensitivity of papillary thyroid carcinoma to vemurafenib [ Cell Death Dis, 2022, 13(2):124] PubMed: 35136031
Effect of Exosomal APE1 on Sensitivity of NSCLC A549 Cells to Cisplatin [ Cancer Research on Prevention and Treatment, 2020, (7): 492-497] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.