| Bioactivity | E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities[1][2][3][4][5]. | ||||||||||||
| Target | Ape-1, Ref-1 | ||||||||||||
| Invitro | E3330 (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs[1].E3330 (0-5 μM) reduces secreted and intracellular VEGF (vascular endothelial growth factor) expression by pancreatic cancer cells, while concomitantly downregulating the cognate receptor Flk-1/KDR on PCECs[1].E3330 (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31+ cells of endothelial lineage[1].E3330 (0-50 µM, 72 h) decreases cell viability in H1975 cells about 45% at 50 µM[2].E3330 (0-30 µM) inhibits the growth and migration of pancreatic cancer cells[3].E3330 (0-30 µM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells[3]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | E3330 (25 mg/kg, Orally, 5 daily, five days each week for three weeks) is neuroprotective against cisplatin-induced alterations in capsaicin-induced vasodilation[4].E3330 (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge[5]. Animal Model: | ||||||||||||
| Name | E3330 | ||||||||||||
| CAS | 136164-66-4 | ||||||||||||
| Formula | C21H30O6 | ||||||||||||
| Molar Mass | 378.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |