| Bioactivity | FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp[1]. |
| Invitro | FM04 抑制 P-糖蛋白的 EC50=83 nM，这里的 EC50 值是指在 P-gp 过表达细胞系 LCC6MDR 中，紫杉醇 (PTX) 降低一半的有效调制剂浓度 IC50 (=3.8 nM)[1]。FM04 (100 μM) 在 LCC6MDR 细胞中表现出与其光亲和衍生物 XC4 的竞争[1]。 |
| Name | FM04 |
| CAS | 1807320-40-6 |
| Formula | C26H25NO4 |
| Molar Mass | 415.48 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liu Z, et al. Identification of Binding Sites in the Nucleotide-Binding Domain of P-Glycoprotein for a Potent and Nontoxic Modulator, the Amine-Containing Monomeric Flavonoid FM04. J Med Chem. 2023 Apr 25. |