| Description | 4,5-Dimethoxycanthin-6-one is an alkaloid isolated from Picrasma quassioides BENNET (Simaroubaceae).4,5-Dimethoxycanthin-6-one was isolated from Picrasma quassioides BENNET (Simaroubaceae) with antimicrobial activity.4,5-Dimethoxycanthin-6-one was isolated from Picrasma quassioides BENNET (Simaroubaceae) with antimicrobial activity. Dimethoxycanthin-6-one is a potent, non-competitive inhibitor of CYP1A2-mediated phenacetin O-deethylation (IC50: 1.7 μM, Ki: 2.6 μM), and a potent inhibitor of cyclic adenosine monophosphate (cAMP) phosphodiesterase.4,5-(4,5-Dimethoxycanthin-6-one) is an alkaloid isolated from Picrasma quassioides BENNET (Simaroubaceae). 4,5-Dimethoxycanthin-6-one has antimicrobial activity against Staphylococcus aureus and its drug-resistant strains.4,5-Dimethoxycanthin-6-one is cytotoxic to the tumor cell lines U937 and HepG2.4,5-Dimethoxycanthin-6-one is a cytotoxicity inhibitor (IC50 : Ki : 6 μM, Ki : 6 μM). |
| In vitro | 4,5-Dimethoxycanthin-6-one 显示出针对 CYP1A2 媒介的 phenacetin O-deethylation 强而非竞争性的抑制作用，其 IC50 值为 1.7μM，Ki 值为 2.6 μM。[2] |
| Target activity | CYP1A2:2.6 μM (Ki), CYP1A2:1.7 μM |
| Synonyms | Methylnigakinone |
| molecular weight | 280.28 |
| Molecular formula | C16H12N2O3 |
| CAS | 18110-87-7 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 9.0 mg/mL (32.1 mM), Sonication is recommended. |
| References | 1. OHMoTo T, et al. Studies on the constituents of Picrasma quassioides BENNET. III. The alkaloidal constituents. Chemical and pharmaceutical bulletin. 1984;32(9): 3579-3583. 2. Miao X, et al. In vitro metabolism of 4, 5-dimethoxycanthin-6-one by human liver microsomes and its inhibition on human CYP1ALife Sci. 2017;190:46-51. 3. Li W, et al. 4,5-Dimethoxycanthin-6-one is a novel LSD1 inhibitor that inhibits proliferation of glioblastoma cells and induces apoptosis and pyroptosis. Cancer Cell Int. 2022;22(1):32. |