产品描述
GSK2593074A is a necroptosis inhibitor for dual-targeting to both RIP1 and RIP3.
体外活性
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.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.
体内活性
GSK2593074A significantly decreases the extent of aortic expansion.GSK2593074A ?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 as well as a reduced abdominal aortic aneurysm ?incidence (from 83.3 to 16.7%).
Cas No.
1337531-06-2
分子式
C27H23N5OS
分子量
465.57
别名
GSK'074;GSK2593074A
储存和溶解度
DMSO:41.67 mg/mL (89.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years