1337531-06-2
1337531-06-2 structure
- Name: GSK2593074A
- Chemical Name: GSK2593074A
- CAS Number: 1337531-06-2
- Molecular Formula: C27H23N5OS
- Molecular Weight: 465.57
- Catalog: Signaling Pathways Apoptosis RIP kinase
- Create Date: 2019-06-04 23:04:34
- Modify Date: 2024-01-10 13:33:41
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GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1].
| Name | GSK2593074A |
|---|
| Description | GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3[1]. |
|---|---|
| Related Catalog | |
| Target |
RIP1, RIP3[1] |
| 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[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 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) [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. |
| References |
| Molecular Formula | C27H23N5OS |
|---|---|
| Molecular Weight | 465.57 |