GSK840
Based on 1 publication(s) in Google Scholar
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
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- Pureza: 99.95%
- No. CAS: 2361146-30-5
- Fòrmula: C21H23N3O3
- Peso molecular:365.43
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GSK840
More
Actividad biológica
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RIPK3 |
GSK840 (GSK'840) (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner[1].
GSK840 binds the kinase domain and inhibits kinase activity with high specificity, targeting a broader range of pro-necrotic stimuli than can be achieved with RIP1 kinase inhibitors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human HT-29 cells (TNF 10 ng/ml + zVAD-fmk 20 μM + SMAC007 100 nM)
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Concentration:0.01-3 μM
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Incubation Time:24 hours
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Result:Blocked TNF-induced necroptosis in a concentration-dependent manner.
Chemical Information
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No. CAS 2361146-30-5
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Appearance Solid
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Peso molecular 365.43
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Fòrmula C21H23N3O3
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Color White to yellow
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SMILES
O=C(OC(C)(C)C)CC1=CC=C(N2C3=CC=C(C(NC)=O)C=C3N=C2)C=C1
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Synonyms
GSK'840
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Loss of Ripk3 attenuated neutrophil accumulation in a lipopolysaccharide-induced zebrafish inflammatory model. [Abstract]2022 Feb 26;8(1):88. PMID: 35220408
Solvente y solubilidad
DMSO : 100 mg/mL (273.65 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (6.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7365 mL | 13.6825 mL | 27.3650 mL | 68.4126 mL |
| 5 mM | 0.5473 mL | 2.7365 mL | 5.4730 mL | 13.6825 mL | |
| 10 mM | 0.2737 mL | 1.3683 mL | 2.7365 mL | 6.8413 mL | |
| 15 mM | 0.1824 mL | 0.9122 mL | 1.8243 mL | 4.5608 mL | |
| 20 mM | 0.1368 mL | 0.6841 mL | 1.3683 mL | 3.4206 mL | |
| 25 mM | 0.1095 mL | 0.5473 mL | 1.0946 mL | 2.7365 mL | |
| 30 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2804 mL | |
| 40 mM | 0.0684 mL | 0.3421 mL | 0.6841 mL | 1.7103 mL | |
| 50 mM | 0.0547 mL | 0.2737 mL | 0.5473 mL | 1.3683 mL | |
| 60 mM | 0.0456 mL | 0.2280 mL | 0.4561 mL | 1.1402 mL | |
| 80 mM | 0.0342 mL | 0.1710 mL | 0.3421 mL | 0.8552 mL | |
| 100 mM | 0.0274 mL | 0.1368 mL | 0.2737 mL | 0.6841 mL |
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