GSK2593074A (GSK'074) 是一种程序性坏死 (necroptosis) 抑制剂, 抑制 RIP1 和 RIP3。
| Cas No. | 1337531-06-2 |
| 别名 | GSK'074 |
| 分子式 | C27H23N5OS |
| 分子量 | 465.57 |
| 溶解度 | DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GSK2593074A (GSK'074) is anecroptosisinhibitor with dual targeting ability to bothRIP1andRIP3[1]. 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 IC50of ~3 nM[1]. Cell Viability Assay[1] | Cell 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 IC50of 3 nM. |
GSK2593074A (GSK'074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated toApoe-/-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)[1]. | Animal Model: | Apoe-/-female mice (9-10 months)[1] | | Dosage: | 0.93 mg/kg/day; 200 µL | | Administration: | Daily i.p. injection; 14 or 28 days | | Result: | Inhibited aneurysm formation in mouse models of aneurysms. |
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