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GSK2593074A

CAS No. : 1337531-06-2

MCE 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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