GSK620
Based on 1 publication(s) in Google Scholar
GSK620, a chemical probe, is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
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- Pureza: 99.79%
- No. CAS: 2088410-46-0
- Fòrmula: C18H19N3O3
- Peso molecular:325.36
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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
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Publications Citing Use of MedChemExpress (MCE) GSK620
More
Actividad biológica
GSK620 shows an anti-inflammatory phenotype in human whole blood. Human blood samples are stimulated with LPS, which produces a strong immune response. The monocyte chemattractant protein 1 (MCP-1/CCL2) is measured. This is a chemokine which recruits monocytes, memory T cells, and dendritic cells to sites of inflammation. GSK620 reduces the MCP-1 response in a concentration-dependent manner with (an expected) ～1 log drop off in potency relative to the biochemical BRD4 BD2 potencies observed[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2088410-46-0
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Appearance Solid
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Peso molecular 325.36
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Fòrmula C18H19N3O3
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Color White to off-white
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SMILES
O=C(C1=CC(C(NC2CC2)=O)=CN(CC3=CC=CC=C3)C1=O)NC
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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J Leukoc Biol
BET inhibition curbs macrophage inflammation, lipid accumulation, and atherogenesis by disrupting the YAP/TAZ-BRD4 axis. [Abstract]2026 Apr 29:qiag017. PMID: 42054500
Solvente y solubilidad
DMSO : 33.33 mg/mL (102.44 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 3.33 mg/mL (10.23 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 3.0735 mL | 15.3676 mL | 30.7352 mL | 76.8380 mL |
| 5 mM | 0.6147 mL | 3.0735 mL | 6.1470 mL | 15.3676 mL | |
| 10 mM | 0.3074 mL | 1.5368 mL | 3.0735 mL | 7.6838 mL | |
| 15 mM | 0.2049 mL | 1.0245 mL | 2.0490 mL | 5.1225 mL | |
| 20 mM | 0.1537 mL | 0.7684 mL | 1.5368 mL | 3.8419 mL | |
| 25 mM | 0.1229 mL | 0.6147 mL | 1.2294 mL | 3.0735 mL | |
| 30 mM | 0.1025 mL | 0.5123 mL | 1.0245 mL | 2.5613 mL | |
| 40 mM | 0.0768 mL | 0.3842 mL | 0.7684 mL | 1.9209 mL | |
| 50 mM | 0.0615 mL | 0.3074 mL | 0.6147 mL | 1.5368 mL | |
| 60 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.2806 mL | |
| 80 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9605 mL | |
| 100 mM | 0.0307 mL | 0.1537 mL | 0.3074 mL | 0.7684 mL |
GSK620 Related Classifications
HY-137892 Related Classifications
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