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Liproxstatin-1 is a specific small molecule ferroptosis inhibitor (IC50=22 nM) via inactivation of the ferroptosis regulator Gpx4 (glutathione peroxidase 4), shows no activity on necroptosis; prevents BODIPY 581/591 C11 oxidation in Gpx4−/− cells, does not interfere with other classical types of cell death, such as TNFα-induced apoptosis and H2O2-induced necrosis; suppresses ferroptosis in Gpx4(-/-) mice, and in a pre-clinical model of ischaemia/reperfusion-induced hepatic damage.




YAP1 inhibitor CA3 (CA3;CIL56) is a small molecule that has remarkable inhibitory activity on YAP1/Tead transcriptional activity; also demonstrates strong inhibitory effects on esophageal adenocarcinoma cell growth especially on YAP1 high-expressing esophageal adenocarcinoma cells both in vitro and in vivo; can effectively suppress radiation-resistant cancer stem cell (CSC) properties and aggressive phenotype by inhibiting proliferation, inducing apoptosis, reducing tumor sphere formation; synergistically inhibits cancer cell growth combined with 5-FU; triggers nonapoptotic cell death, a potent and selective probe of ferroptosis; stimulates the activity of ACC1, inhibits the normal breakdown of fatty acids by mitochondrial β-oxidation.


Piperazine Erastin


Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death.


Imidazole ketone erastin

1801530-11-9 Imidazole ketone erastin (IKE, Ferroptosis inducer IKE) is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications; potently reduces DLBCL cell number with IC50 of <100 nM (SUDHL6 cell IC50=1 nM); exerts antitumor effect by inhibiting system xc-, leading to glutathione depletion (GSH depletion IC50=34 nM, SUDHL6 cells), lipid peroxidation, and the induction of ferroptosis biomarkers both in vitro and in vivo, induced lipid peroxidation in tumor tissue.


1467047-25-1 SRS11-92 (SRS 11-92) is a small molecule inhibitor of Ferroptosis and a derivative of Ferrostatin-1 (Fer-1), inhibits ferroptotic cell death induced by erastin in HT-1080 human fibrosarcoma cells with EC50 of 6 nM; inhibits iron-induced cell death in isolated mouse kidney proximal tubules at 2 uM, and fully protects rat oligodendrocytes from cystine deprivation-induced cell death in an in vitro model of periventricular leukomalacia when used at a concentration of 100 nM; also increases survival of medium spiny neurons in rat corticostriatal brain slices in an in vitro model of Huntington’s disease in a concentration-dependent manner.


347174-05-4 Ferrostatin-1 is a potent ferroptosis inhibitor with IC50 of 33 nM, inhibits erastin-induced ferroptosis in HT-1080 cells with EC50 of 60 nM; prevents erastin-induced accumulation of cytosolic and lipid ROS, does not inhibit ERK phosphorylation or arrest the proliferation of HT-1080 cells.


UAMC-3203 is a novel potent, drug-like ferroptosis inhibitor with IC50 of 12 nM, inhibit erastin-induced ferroptotic cell death more potently than Ferrostatin-1; shows an improved protection compared to Fer-1 against multi-organ injury in mice, represents novel lead compounds with therapeutic potential in relevant ferroptosis-driven disease models.

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