gpx4-in-2

GPX4-IN-2 is a potent inhibitor of GPX4, exhibiting antiproliferative activity and holding potential for cancer research applications.

GPX4 Activator 2 (Compound C3) serves as an activator of GPX4 and exhibits cardioprotective effects by inhibiting cellular iron death (ferroptosis) with an efficacy concentration (EC50) of 7.8 μM. It is used in the study of myocardial damage.

IRF1-IN-2 (Compound I-19) is an inhibitor of IRF1. It reduces the recruitment of IRF1 to the CASP1 promoter and hinders cell death signaling pathways by inhibiting the cleavage of Caspase 1, GSDMD, IL-1, and PARP1, as well as by preventing the phosphorylation of TKB1. The compound also upregulates GPX4 and downregulates FACL4. Additionally, IRF1-IN-2 provides protective effects against skin inflammatory damage induced by ionizing radiation.

QD-394 is an inducer of reactive oxygen species (ROS) production.1It induces lipid peroxidation, increases in intracellular accumulation of reactive oxygen species (ROS), and decreases in the reduced glutathione (GSH) to oxidized GSH (GSSG) ratio in MIA PaCa-2 pancreatic cancer cells when used at concentrations ranging from 0.5 to 10 μM. QD-394 is cytotoxic to MIA PaCa-2, PANC-1, and BxPC-3 cancer cells (IC50s = 0.64, 0.34, and 0.9 μM, respectively). QD-394 acts synergistically with napabucasin to reduce colony formation in MIA PaCa-2 cells. 1.Hu, S., Sechi, M., Singh, P.K., et al.A novel redox modulator induces a GPX4-mediated cell death that is dependent on iron and reactive oxygen speciesJ. Med. Chem.63(17)9838-9855(2020)

1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE is a phospholipid with stearic acid at the sn-1 position and 15(S)-HpETE at the sn-2 position, produced by oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-lipoxygenase (15-LO). At concentrations of 0.6 and 0.9 μM, it increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080 cells [1].