FM04 

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].

FM04 exhibits the EC₅₀=83 nM for inhibiting P-glycoprotein, while the EC₅₀ value refers to effective concentration of the modulator at which the IC₅₀ (=3.8 nM) of paclitaxel (PTX) in the P-gp overexpressing cell line LCC6MDR can be reduced by half^[1].
FM04 (100 μM) shows competition with its photoaffinity derivative XC4 in LCC6MDR cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

415.48

C₂₆H₂₅NO₄

1807320-40-6

Solid

White to off-white

O=C1C=C(C2=CC=C(OCCOCCNCC3=CC=CC=C3)C=C2)OC4=C1C=CC=C4

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]