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]}. IC50 & Target:Ape-1, Ref-1^[1] In Vitro:Erenapursta (E3330) (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs^[1].
Erenapursta (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].
Erenapursta (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31⁺ cells of endothelial lineage^[1].
Erenapursta (0-50 μM, 72 h) decreases cell viability in H1975 cells about 45% at 50 μM^[2].
Erenapursta (0-30 μM) inhibits the growth and migration of pancreatic cancer cells^[3].
Erenapursta (0-30 μM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells^[3]. In Vivo:Erenapursta (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].
Erenapursta (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge^[5].