beta-Lapachone (ARQ-501, CO-501)

Biological Activity

Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only. For the detailed information of beta-Lapachone (ARQ-501, CO-501), the solubility of beta-Lapachone (ARQ-501, CO-501) in water, the solubility of beta-Lapachone (ARQ-501, CO-501) in DMSO, the solubility of beta-Lapachone (ARQ-501, CO-501) in PBS buffer, the animal experiment (test) of beta-Lapachone (ARQ-501, CO-501), the cell expriment (test) of beta-Lapachone (ARQ-501, CO-501), the in vivo, in vitro and clinical trial test of beta-Lapachone (ARQ-501, CO-501), the EC50, IC50,and affinity,of beta-Lapachone (ARQ-501, CO-501), Please contact DC Chemicals.

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.