1807320-40-6

1807320-40-6 structure

Name: FM04
Chemical Name: FM04
CAS Number: 1807320-40-6
Molecular Formula: C₂₆H₂₅NO₄
Molecular Weight: 415.48
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
Create Date: 2023-08-26 11:01:00
Modify Date: 2024-01-13 11:11:31
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].

Name	FM04

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein
In Vitro	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]。
References	[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.

Molecular Formula	C₂₆H₂₅NO₄
Molecular Weight	415.48