Ferroptosis inducer-12

Ferroptosis inducer-12 is a potent and selective ferroptosis inducer. Ferroptosis inducer-12 exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC₅₀ values of 3 nM and 5 nM, respectively. Ferroptosis inducer-12 strongly inhibits GPX4 enzymatic activity, induces intracellular ROS and elevates intracellular Fe 2+ levels in OS-RC-2 cells. Ferroptosis inducer-12 significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. Ferroptosis inducer-12 can be used for the study of cancer ^[1].

In Vivo, Ferroptosis inducer-12 (Compound A6) (25-50 mg/kg, i.p., once every 3 days for 27 days) significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts^[1].

In Vitro, Ferroptosis inducer-12 (Compound A6) (48 h) exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC₅₀ values of 3 nM (HT1080) and 5 nM (OS-RC-2)^[1]. Ferroptosis inducer-12 (1 μM, 2 h) strongly inhibits glutathione peroxidase 4 (GPX4) enzymatic activity in OS-RC-2 cells^[1]. Ferroptosis inducer-12 (0.5 μM, 4 h) induces intracellular ROS, elevates intracellular Fe2+ levels and promotes lipid peroxidation (LPO) accumulation in OS-RC-2 cells^[1]. Ferroptosis inducer-12 (10 nM, 24 h) significantly suppresses migration and reduces invasive capacity of OS-RC-2 cells^[1].

References:
[1]. Wang J, et al. Structural optimization and biological evaluation of ferrocene-appended RSL3 derivatives as potent ferroptosis inducers. Eur J Med Chem. 2025 Sep 16;301:118162.