SGK1-IN-10
SGK1-IN-10 is an ATP-competitive SGK1 inhibitor with an IC50 of 2.53 μM against human SGK1, and it exhibits blood-brain barrier permeability. SGK1-IN-10 downregulates the phosphorylation levels of MDM2 and GSK-3β, induces apoptosis and inhibits cell migration. SGK1-IN-10 can be used in the research of prostate 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。
- 分子式: C24H27F3N4O
- 分子量:444.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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SGK1 2.53 μM (IC50) |
SGK1-IN-10 (compound 7h) inhibits proliferation of PC3 prostate cancer cells with an IC50 of 1.08 μM and LNCaP prostate cancer cells with an IC50 of 1.24 μM[1].
SGK1-IN-10 inhibits proliferation of HepG2 liver cancer cells with an IC50 of 1.21 μM and shows low cytotoxicity to LX2 normal liver cells with an IC50 of 10.07 μM, yielding a selectivity index of 9.15[1].
SGK1-IN-10 (0.5-2.0 μM; 48 h) induces concentration-dependent apoptosis in PC3 prostate cancer cells, with a total apoptotic rate of 74.70% at 2.0 μM[1].
SGK1-IN-10 (0.5-2.0 μM; 48 h) induces concentration-dependent S-phase cell cycle arrest in PC3 prostate cancer cells, with 61.48% of cells in S-phase at 2.0 μM[1].
SGK1-IN-10 (0.5-2.0 μM; 24-48 h) inhibits migration of PC3 prostate cancer cells in a dose- and time-dependent manner[1].
SGK1-IN-10 (0.01-10 μM; 2 h) directly binds to and stabilizes SGK1 protein in PC3 prostate cancer cells in a temperature- and concentration-dependent manner[1].
SGK1-IN-10 (0.5-2.0 μM) dose-dependently inhibits phosphorylation of SGK1 substrates MDM2 and GSK-3β in PC3 prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 prostate cancer cells
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Concentration:0.5 μM, 1.0 μM, 2.0 μM
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Incubation Time:48 h
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Result:Increased total apoptotic rate to 19.64% at 0.5 μM compared to 5.97% in DMSO control.
Increased total apoptotic rate to 28.19% at 1.0 μM compared to 5.97% in DMSO control.
Increased total apoptotic rate to 74.70% at 2.0 μM compared to 5.97% in DMSO control.
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Cell Line:PC3 prostate cancer cells
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Concentration:0.5 μM, 1.0 μM, 2.0 μM
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Incubation Time:48 h
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Result:Increased S-phase population to 49.59% at 0.5 μM compared to 22.60% in DMSO control.
Increased S-phase population to 59.40% at 1.0 μM compared to 22.60% in DMSO control.
Increased S-phase population to 61.48% at 2.0 μM compared to 22.60% in DMSO control.
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Cell Line:PC3 prostate cancer cells
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Concentration:0.5 μM, 1.0 μM, 2.0 μM
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Incubation Time:24 h, 48 h
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Result:Inhibited wound closure in a dose- and time-dependent manner.
Showed significant inhibition at all concentrations at 24 h compared to DMSO control.
Showed significant inhibition at all concentrations at 48 h compared to DMSO control.
化学情報
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分子量 444.49
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分子式 C24H27F3N4O
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SMILES
FC(C1=CC(NC2=CC=C(CN3C[C@H](C)N[C@H](C)C3)C=C2)=NC4=CC=C(OC)C=C14)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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