Drug intelligence / Profile preview

RSL3

Development stage
Preclinical
Modality
Small Molecules
01

Overview

RSL3 is a small molecule ferroptosis activator and a potent, selective inhibitor of glutathione peroxidase 4 (GPX4). By directly binding to and inactivating GPX4, an essential enzyme for reducing lipid peroxides and maintaining cellular redox balance, RSL3 induces ferroptosis—a form of regulated cell death characterized by iron-dependent accumulation of lipid reactive oxygen species. Originally identified as selectively lethal to oncogenic-RAS-harboring tumor cells, it has since been shown to induce rapid non-apoptotic cell death in various cancer cell lines regardless of their RAS mutation status. Its primary use is as a research tool for studying ferroptosis mechanisms and potential anticancer strategies[1][2][4][5].

Other names
RAS-selective lethal 3(1S,3R)-RSL3
02

Targets

GPX4 (Glutathione peroxidase 4)

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