Drug intelligence / Profile preview

erastin2

Development stage
Preclinical
Lead developer
Columbia University
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Erastin2 is a potent small molecule and a selective inhibitor of the system xc- cystine/glutamate antiporter. It is a more potent and soluble analog of the original ferroptosis-inducing compound, erastin. By blocking the exchange of extracellular cystine for intracellular glutamate, erastin2 depletes cellular glutathione (GSH) levels, which in turn inactivates the lipid repair enzyme glutathione peroxidase 4 (GPX4). This cascade leads to the lethal accumulation of iron-dependent lipid peroxides, triggering a form of regulated necrotic cell death known as ferroptosis. Erastin2 is primarily utilized as a pharmacological research tool to investigate the mechanisms of ferroptosis and has shown potential in preclinical studies for treating various cancers, such as glioblastoma, and for inhibiting the replication of certain viruses like the bovine viral diarrhea virus (BVDV) by modulating host redox homeostasis.

02

Targets

SLC7A11 (Cystine-Glutamate Antiporter)SLC3A2 (Solute carrier family 3 member 2)

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