TfR-1-IN-1 (compound C4) is an inhibitor of transferrin receptor 1 (TfR-1) with anticancer activity. TfR-1-IN-1 strongly increases intracellular iron (II) levels as a driving force for the induction of ferroptosis. TfR-1-IN-1 significantly reduces the metabolic activity of ovarian cancer (A2780cis), breast cancer (MDA-MB 231), and leukemia (HL-60) cell lines with IC50 values of 0.51, 0.46, and 0.48 μM, respectively.
References:
[1]. Bernkop-Schnürch, et al. Transferrin Receptor-Mediated Cellular Uptake of Fluorinated Chlorido [N, N′-bis (salicylidene)-1, 2-phenylenediamine] iron (III) Complexes. ACS Omega (2024).