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GSK2593074A

CAS No. : 1337531-06-2

MCE 国际站：GSK2593074A

产品活性：GSK2593074A (GSK’074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。

研究领域：Apoptosis

作用靶点：RIP kinase

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 IC₅₀~3 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 IC₅₀ 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<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05) .

相关产品：Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | NF-κB Signaling Compound Library | Necrostatin-1 | GSK-872 | GSK583 | GSK840 | GSK-843 | HS-1371 | RIP2 kinase inhibitor 2 | PROTAC RIPK degrader-2 | RIPK-IN-4 | RIPK1-IN-4 | RIPK1-IN⁻⁷ | PROTAC RIPK degrader-6 | Kongensin A | GNE684 | cRIPGBM

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