| Description | Quercetagetin (6-Hydroxyquercetin) (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu. It is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50: 0.34 μM). |
| In vitro | Quercetagetin抑制了PIM2、PKA和RSK2（IC50值分别为3.45、21.2和2.82 μM）。在72小时内，Quercetagetin（0.1、1、10和100 μM）抑制了RWPE2前列腺癌细胞的生长，平均ED50为3.8 μM [2]。 |
| In vivo | Quercetagetin 显著抑制 UVB 引起的皮肤癌发展。通过局部给小鼠皮肤施用 4 或 20 nmol Quercetagetin，可分别将肿瘤发生率降低 32.0% 和 46.7% [3]。 |
| Cell experiments | Cell Line: RWPE2 prostate cancer cells. Concentration: 0.1, 1, 10, and 100 μM. Incubation Time: 72 hours [2] |
| Animal experiments | Animal Model: SKH-1 hairless mice model. Dosage: 4 or 20 nmol. Administration: Topical application; 28 weeks [3] |
| Target activity | Pim1:0.34 μM, Pim2:3.5 μM |
| Synonyms | 栎草亭, 6-Hydroxyquercetin |
| molecular weight | 318.24 |
| Molecular formula | C15H10O8 |
| CAS | 90-18-6 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (392.79 mM) |
| References | 1. Yang X, et al. Isolation and identification of an antioxidant flavonoid compound from citrus-processing by-product. J Sci Food Agric. 2011 Aug 15;91(10):1925-7. 2. Holder S, et al. Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase. Mol Cancer Ther. 2007 Jan;6(1):163-72. 3. Baek S, et al. Structural and functional analysis of the natural JNK1 inhibitor quercetagetin. J Mol Biol. 2013 Jan 23;425(2):411-23. |