Molecular Formula | C15H14O3
|
Molar Mass | 242.27 |
Density | 1.25±0.1 g/cm3(Predicted) |
Melting Point | >110°C (dec.) |
Boling Point | 381.4±42.0 °C(Predicted) |
Solubility | Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 15 mg/ml) |
Appearance | Orange to brown solid. |
Color | Orange |
Storage Condition | Inert atmosphere,Room Temperature |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.、 |
In vitro study | Beta-Lapachone inhibited DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. Beta-lapacone (100 nM or higher) treatment inhibited Topo I DNA stretching activity by more than 95% compared with the control group. Beta-Lapachone(1-5 μm) acts on HL-60 and three prostate cancer (DU-145, PC-3, and LNCaP) cells to arrest the cell cycle at the G0/G1 phase, and induce apoptosis by locking Topo I on DNA and preventing replication fork movement. Beta-Lapachone acts on mouse 3T3 fibroblasts and human endothelial cells EAhy926 cells in vitro to promote cell migration through different MAPK signaling pathways, thereby accelerating wound healing. In addition, Beta-Lapachone non-competitive inhibition of purified recombinant IDO1 activity, IC50 was 0.44 μm, Beta-Lapachone also inhibited intracellular IDO1 inhibitory activity, IC50 was 1.0 μm, it is partly dependent on biotransformation by NQO1. Beta-Lapachone induces programmed necrosis of NQO1 + cancer cells through nqo1-dependent formation of reactive oxygen species (ROS) and PARP1 overactivation. |
In vivo study | Beta-Lapachone A mouse model of human ovarian cancer xenografts at a dose of 50 mg/kg can effectively inhibit tumor growth in vivo, and Beta-Lapachone combined with Taxol can Synergistically Induce cell apoptosis. Beta-Lapachone treatment of normal and diabetic (db/db) mice accelerated the healing process compared to the blank control group. |