[CAS NO. 1337531-06-2] GSK2593074A
PRODUCTS SPECIFICATIONS [1337531-06-2]
DESCRIPTION [1337531-06-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 465.57 |
| Molecular Formula | C27H23N5OS |
| SMILES | CN1N=CC(C2=CN=C(N)C3=C2SC=C3C4=CC5=C(N(C(CC6=CC=CC=C6)=O)CC5)C=C4)=C1 |
Summary
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3 [1] .
IC50 & 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 IC 50 ~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 IC 50 of ~3 nM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 41.67 mg/mL ( 89.50 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1479 mL | 10.7395 mL | 21.4790 mL |
| 5 mM | 0.4296 mL | 2.1479 mL | 4.2958 mL |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1479 mL |
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