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MedChemExpress - Model E3330 - ...

MedChemExpress - Model E3330 - 136164-66-4

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].

E3330

MCE China：E3330

Brand：MedChemExpress (MCE)

Cat. No.HY-19357

CAS：136164-66-4

Synonyms：APX-3330

Purity：99.34%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

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].

IC50 & Target：Ape-1, Ref-1[1] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> E3330 Related Antibodies Cell Proliferation Assay[1] Cell Line: Human umbilical vein endothelial cells (HUVECs), murine pancreatic cancer associated endothelial cells (mPCECs), human endothelial progenitor cells (hEPCs)

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Brand introduction:
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