GNE684
Based on 1 Customer Validation
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.
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- Pureza: 99.08%
- No. CAS: 2438637-64-8
- Fòrmula: C23H24N6O3
- Peso molecular:432.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
IC50: 21 nM (human RIP1), 189 nM (mouse RIP1), 691 nM (rat RIP1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H9c2 | IC50 |
154 nM
Compound: GNE684; 54
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Inhibition of TNF induced necroptosis cell death in rat H9c2 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
Inhibition of TNF induced necroptosis cell death in rat H9c2 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
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[PMID: 36346971] |
| HT-29 | IC50 |
6.6 nM
Compound: GNE684; 54
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Inhibition of TNF induced necroptosis cell death in human HT-29 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
Inhibition of TNF induced necroptosis cell death in human HT-29 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
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[PMID: 36346971] |
| L929 | IC50 |
81 nM
Compound: GNE684; 54
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Inhibition of TNF induced necroptosis cell death in mouse L929 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
Inhibition of TNF induced necroptosis cell death in mouse L929 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6
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[PMID: 36346971] |
GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines[1].
GNE684 (20 μM; 0-60 minutes) disrupts TBZ (2 μM BV6, 20 ng/ml TNF, 20 μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L929 cells, Jurkat cells, MEFs
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Concentration:20 μM
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Incubation Time:20 hours
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Result:Inhibited RIP1 kinase driven cell death effectively in several human and mouse cell lines.
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Cell Line:HT-29 cells, J774A.1 cells
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Concentration:0 μM, 20 μM
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Incubation Time:0 minute, 15 minutes, 60 minutes
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Result:Disrupted TBZ (2 μM BV6, 20 ng/ml TNF, 20μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.
GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nemofl/fl Villin.creERT2 mice (NEMO IEC-KO)[1]
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Dosage:50 mg/kg
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Administration:Oral administration; twice daily; from days 2–6 treated with tamoxifen
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Result:Almost completely protected the NEMO-deficient intestines from colitis and ileitis.
Chemical Information
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No. CAS 2438637-64-8
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Appearance Solid
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Peso molecular 432.48
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Fòrmula C23H24N6O3
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Color White to off-white
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SMILES
COC1=NC=C(N(C)C([C@@H](NC(C2=NN([C@H](C3=CC=CC=C3)CC4)C4=N2)=O)CC5)=O)C5=C1
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (231.22 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: ≥ 5 mg/mL (11.56 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.56 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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)
- 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 | 2.3122 mL | 11.5612 mL | 23.1225 mL | 57.8061 mL |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6245 mL | 11.5612 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 mL | 5.7806 mL | |
| 15 mM | 0.1541 mL | 0.7707 mL | 1.5415 mL | 3.8537 mL | |
| 20 mM | 0.1156 mL | 0.5781 mL | 1.1561 mL | 2.8903 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL | 2.3122 mL | |
| 30 mM | 0.0771 mL | 0.3854 mL | 0.7707 mL | 1.9269 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5781 mL | 1.4452 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9634 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7226 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5781 mL |
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