GSK2593074A
Based on 2 publication(s) in Google Scholar
GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.07%
- No. CAS: 1337531-06-2
- Fòrmula: C27H23N5OS
- Peso molecular:465.57
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK2593074A
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Actividad biológica
Descripciòn
IC50 & Target
RIP1, RIP3[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.03 μM
Compound: 21
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Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
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[PMID: 22827572] |
| L929 | IC50 |
3 nM
Compound: GSK2593074A; 18
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Anti-necroptic activity in mouse L929 cells incubated for 3 hrs in presence of TNF alpha/zVAD by celltiter-glo assay
Anti-necroptic activity in mouse L929 cells incubated for 3 hrs in presence of TNF alpha/zVAD by celltiter-glo assay
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[PMID: 36346971] |
| MOVAS-1 | IC50 |
3 nM
Compound: GSK2593074A; 18
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Anti-necroptic activity in mouse MOVAS cells incubated for 6 hrs in presence of TNF alpha/zVAD by celltiter-glo assay
Anti-necroptic activity in mouse MOVAS cells incubated for 6 hrs in presence of TNF alpha/zVAD by celltiter-glo assay
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[PMID: 36346971] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929
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Concentration:0.01, 0.1, 1, 10, and 100 nM
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Incubation Time:6 hours for MOVAS cells; 3 hours for L929 cells
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Result:Inhibited MOVAS and L929 cells with the IC50 of 3 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Apoe-/- female mice (9-10 months)[1]
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Dosage:0.93 mg/kg/day; 200 µL
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Administration:Daily i.p. injection; 14 or 28 days
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Result:Inhibited aneurysm formation in mouse models of aneurysms.
Chemical Information
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No. CAS 1337531-06-2
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Appearance Solid
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Peso molecular 465.57
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Fòrmula C27H23N5OS
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Color Light yellow to khaki
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SMILES
CN1N=CC(C2=CN=C(N)C3=C2SC=C3C4=CC5=C(N(C(CC6=CC=CC=C6)=O)CC5)C=C4)=C1
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Synonyms
GSK'074
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2026 Apr 1;17(1):4716. PMID: 41922346 -
Thromb Haemost
Macrophage ferroptosis promotes MMP2/9 overexpression induced by hemin in hemorrhagic plaque. [Abstract]2024 Jun;124(6):568-580. PMID: 37696298
Solvente y solubilidad
In Vitro:
DMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1479 mL | 10.7395 mL | 21.4790 mL | 53.6976 mL |
| 5 mM | 0.4296 mL | 2.1479 mL | 4.2958 mL | 10.7395 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1479 mL | 5.3698 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4319 mL | 3.5798 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6849 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8592 mL | 2.1479 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7899 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3424 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0740 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL | |
| 80 mM | 0.0268 mL | 0.1342 mL | 0.2685 mL | 0.6712 mL |
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