Kaempferol is an inverse agonist of ERRα and ERRγ that inhibits estrogen receptor (ER α) expression in breast cancer cells and induces apoptosis by activating MEK-MAPK in glioblastoma cells and lung cancer cells. It can be used in breast cancer research.
J Cell Mol Med. 2020 May;24(9):5168-5184.
A network pharmacology-based approach to explore the effects of Chaihu Shugan powder on a non-alcoholic fatty liver rat model through nuclear receptors
Kaempferol purchased from AbMole
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Source | J Cell Mol Med 2020 May. Figure 8. Kaempferol (Abmole Bioscience, USA) |
| Method | HPLC-MS | |
| Cell Lines | - | |
| Concentrations | - | |
| Incubation Time | - | |
| Results | Kaempferol interacts with 3 amino acids, ARG 288, LEU 330 and SER 342, near the PPARγ active site and forms 4 hydrogen bonds, thus promoting binding. Naringenin formed a network of five hydrogen bonds with PPARγ through 4 amino acids, CYS 285, HIS 440, TYR 327 and LEU 340, near the active site, establishing stable binding |
| Molecular Weight | 286.23 |
| Formula | C15H10O6 |
| CAS Number | 520-18-3 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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