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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.86%
- CAS 番号: 1629249-40-6
- 分子式: C29H38ClN5O2
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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MedChemExpress（MCE）の使用を引用している文献 GSK 3008348 hydrochloride
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生物活性
製品説明
IC50 & Target
[3]|
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) |
体外実験
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.
化学情報
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CAS 番号 1629249-40-6
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性状 Solid
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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)
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (394 KB)
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- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
GSK 3008348 hydrochloride 関連分類
HY-19767A 関連分類
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