GSK2593074A

GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3 In Vitro GSK2593074A (GSK’074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC 50 ~3 nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC 50 of ~3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929 Concentration: 0.01, 0.1, 1, 10, and 100 nM Incubation Time: 6 hours for MOVAS cells; 3 hours for L929 cells Result: Inhibited MOVAS and L929 cells with the IC 50 of 3 nM. In Vivo GSK2593074A (GSK’074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe -/- mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P Form:Solid IC50& Target:RIP1, RIP3

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