Erenapurstat

Erenapursta (E3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1) /Ref-1 (redox factor-1) redox. Erenapursta is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. Erenapursta shows anticancer activities[1][2][3][4][5].

Product Specifications

CAS Number

[136164-66-4]

Product Name Alternative

E3330; APX-3330

UNSPSC

12352211

Hazard Statement

H302, H411

Target

AP-1; DNA/RNA Synthesis; HIF/HIF Prolyl-Hydroxylase; NF-κB; Reactive Oxygen Species (ROS) ; VEGFR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/e3330.html

Purity

99.67

Solubility

DMSO : 120 mg/mL (ultrasonic)

Smiles

CCCCCCCCC/C(C(O)=O)=C\C1=C(C)C(C(OC)=C(OC)C1=O)=O

Molecular Formula

C21H30O6

Molecular Weight

378.46

Precautions

H302, H411

References & Citations

[1]Zou GM, et al. The Ape-1/Ref-1 redox antagonist E3330 inhibits the growth of tumor endothelium and endothelial progenitor cells: therapeutic implications in tumor angiogenesis. J Cell Physiol. 2009 Apr;219 (1) :209-18.|[2]Manguinhas R, et al. Impact of the APE1 Redox Function Inhibitor E3330 in Non-small Cell Lung Cancer Cells Exposed to Cisplatin: Increased Cytotoxicity and Impairment of Cell Migration and Invasion. Antioxidants (Basel) . 2020 Jun 24;9 (6) :550.|[3]Zou GM, et al. Small-molecule inhibitor of the AP endonuclease 1/REF-1 E3330 inhibits pancreatic cancer cell growth and migration. Mol Cancer Ther. 2008 Jul;7 (7) :2012-21.|[4]Kelley MR, et al. Role of the DNA base excision repair protein, APE1 in cisplatin, oxaliplatin, or carboplatin induced sensory neuropathy. PLoS One. 2014 Sep 4;9 (9) :e106485.|[5]Nagakawa J, et al. Protective effect of E3330, a novel quinone derivative, in galactosamine-induced hepatitis in rats. J Pharmacol Exp Ther. 1993 Jan;264 (1) :496-500.