| Field | Specification |
|---|---|
| Alternative names | GSK'074 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H23N5OS |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK2593074A, also known as GSK'074, is a necroptosis inhibitor with dual targeting activity against RIP1 and RIP3[1]. It is supplied as a light yellow to khaki solid (C27H23N5OS, MW 465.57) at 99.07% purity.
Physical & Chemical Properties
| CAS Number | 1337531-06-2 |
|---|---|
| Molecular Formula | C27H23N5OS |
| Molecular Weight | 465.57 g/mol |
| Purity | 99.07% |
| Appearance | Solid |
| Color | Light yellow to khaki |
| SMILES | CN1N=CC(C2=CN=C(N)C3=C2SC=C3C4=CC5=C(N(C(CC6=CC=CC=C6)=O)CC5)C=C4)=C1 |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 41.67 mg/mL (89.50 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 41.67 mg/mL (89.50 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (4.47 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
GSK2593074A (GSK’074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) fully protects human and murine cells from necroptosis triggered by different stimuli, with an IC50~3 nM. Across several cell types, among them mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), as well as human colon epithelial cells (HT29), necroptosis is blocked by GSK2593074A 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
In Apoe-/- mice, GSK2593074A (GSK’074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administered right after pump implantation. Relative to the DMSO group, GSK2593074A-treated mice display significantly less aneurysm formation, seen as a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) and a lower abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A also significantly lowers 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Mitochondrial vulnerability underlies myocarditis from COVID-19 mRNA vaccine. Nat Commun 2026 Apr 1;17(1):4716. PMID: 41922346
Macrophage ferroptosis promotes MMP2/9 overexpression induced by hemin in hemorrhagic plaque. Thromb Haemost 2024 Jun;124(6):568-580. PMID: 37696298
