GSK 3008348 hydrochloride
Based on 2 publication(s) in Google Scholar
GSK 3008348 hydrochloride 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 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride 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 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.
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- Pureté: 99.86%
- CAS No.: 1629249-40-6
- Formule: C29H38ClN5O2
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) GSK 3008348 hydrochloride
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Activité biologique
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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 hydrochloride 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 hydrochloride (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 hydrochloride (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.
Chemical Information
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CAS No. 1629249-40-6
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Appearance Solid
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Formule C29H38ClN5O2
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Color Light yellow to khaki
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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.[x].Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvant et solubilité
H2O : 100 mg/mL (Need ultrasonic)
DMSO : 11.66 mg/mL (Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Pureté et documentation
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Fiche technique (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)