Piperazine Erastin

Piperazine Erastin (CAS No.: 1538593-71-3) is a small-molecule research tool derived from the erastin chemical scaffold and is classified as a ferroptosis inducer. It is primarily intended for studies in cancer biology, redox metabolism, and programmed cell death signaling in biomedical research and drug discovery; its functional background is closely associated with early compound screening targeting vulnerabilities in the RAS pathway. Mechanistically, it functionally inhibits the system xc? cystine/glutamate antiporter to reduce cystine uptake, leading to decreased intracellular reduced glutathione levels and secondary attenuation of glutathione peroxidase 4 activity, thereby promoting the accumulation of lipid peroxides and triggering iron-dependent, non-apoptotic cell death; consistent in vitro readouts often include reduced extracellular glutamate efflux and decreased cellular glutathione content. Its in vitro activity typically occurs at submicromolar to low micromolar levels and is influenced by factors such as cell lineage, assay format, and oncogenic signaling background, with higher sensitivity often observed in certain RAS signaling-activated models. In research applications, this compound is used to induce and manipulate ferroptosis for pathway mapping, high-content or high-throughput screening, and target validation. It can be used in various cellular systems and in animal models such as mouse xenografts to investigate ferroptosis-related biological responses without any clinical orientation; experiments commonly employ designs combining time-course and dose-response analyses, with ferroptosis modulators such as iron chelators or lipophilic antioxidants used for rescue or challenge, and are further confirmed through orthogonal indicators such as lipid peroxidation and glutathione status. The specific concentration or dose used depends on the experimental design and research objectives, and this product is for laboratory research and drug discovery use only.