GSK 3008348
Based on 2 publication(s) in Google Scholar
GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.
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- Pureza: 98.04%
- No. CAS: 1629249-33-7
- Fòrmula: C29H37N5O2
- Peso molecular:487.64
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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
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Publications Citing Use of MedChemExpress (MCE) GSK 3008348
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Actividad biológica
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αvβ6 1.50 nM (IC50) |
αvβ1 2.83 nM (IC50) |
αvβ3 12.53 nM (IC50) |
αvβ5 4.00 nM (IC50) |
αvβ8 2.26 nM (IC50) |
GSK 3008348 antagonizes integrin αvβ6 with an affinity (pIC50) value of 8.1 in the fluorescence polarisation assay, whereas its affinity in the cell adhesion assays (K562 cells) is for:αvβ6 (pIC50 = 8.4); αvβ3 (pIC50 = 6); αvβ5 (pIC50 = 6.9); αvβ8 (pIC50 = 7.7)[1].
GSK 3008348 (8 h) suppresses FMDV RNA (vRNA) replication and virus production when added prior to or concurrently with virus infection in PK-15 cells[2].
GSK 3008348 (10 μM, 1 h) decreases TGF-β1-activated procollagen I production in primary human hepatic stellate cells, fails to inhibit TGF-β1 induced SMAD3 and SMAD2 phosphorylation, but inhibits TGF-β-induced phosphorylation of ERK1/2 and STAT3[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hepatic stellate cells
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Concentration:10 μM
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Incubation Time:1 h
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Result:Reversed TGF-β1 induced p-SMAD3 nuclear translocation.
Significantly inhibited TGFβ1 induced ERK1/2 phosphorylation levels.
Significantly inhibited STAT3 phosphorylation in HSCs.
Did not show effects on TGF-β1-induced SMAD3 phosphorylation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1629249-33-7
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Appearance Solid
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Peso molecular 487.64
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Fòrmula C29H37N5O2
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Color Brown to orange
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SMILES
O=C(O)C[C@@H](C1=CC(N2N=C(C)C=C2C)=CC=C1)CN3C[C@H](CCC(N4)=CC=C5C4=NCCC5)CC3
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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 (2)
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Journal Impact Factor
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Most Recent
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mBio
Heat Shock Protein 60 Is Involved in Viral Replication Complex Formation and Facilitates Foot and Mouth Virus Replication by Stabilizing Viral Nonstructural Proteins 3A and 2C. [Abstract]2022 Oct 26;13(5):e0143422. PMID: 36106732 -
Biochem J
Integrin αVβ1 regulates procollagen I production through a non-canonical transforming growth factor β signaling pathway in human hepatic stellate cells. [Abstract]2021 May 14;478(9):1689-1703. PMID: 33876829
Solvente y solubilidad
DMSO : 25 mg/mL (51.27 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 (5.13 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 (5.13 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 (278 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
[2]. Tang J, et al. Heat Shock Protein 60 Is Involved in Viral Replication Complex Formation and Facilitates Foot and Mouth Virus Replication by Stabilizing Viral Nonstructural Proteins 3A and 2C. mBio. 2022 Oct 26;13(5):e0143422. [Content Brief]
[3]. Han Z, et al. Integrin αVβ1 regulates procollagen I production through a non-canonical transforming growth factor β signaling pathway in human hepatic stellate cells. Biochem J. 2021 May 14;478(9):1689-1703. [Content Brief]
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 | 2.0507 mL | 10.2535 mL | 20.5069 mL | 51.2673 mL |
| 5 mM | 0.4101 mL | 2.0507 mL | 4.1014 mL | 10.2535 mL | |
| 10 mM | 0.2051 mL | 1.0253 mL | 2.0507 mL | 5.1267 mL | |
| 15 mM | 0.1367 mL | 0.6836 mL | 1.3671 mL | 3.4178 mL | |
| 20 mM | 0.1025 mL | 0.5127 mL | 1.0253 mL | 2.5634 mL | |
| 25 mM | 0.0820 mL | 0.4101 mL | 0.8203 mL | 2.0507 mL | |
| 30 mM | 0.0684 mL | 0.3418 mL | 0.6836 mL | 1.7089 mL | |
| 40 mM | 0.0513 mL | 0.2563 mL | 0.5127 mL | 1.2817 mL | |
| 50 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0253 mL |
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