LSD1-IN-46
LSD1-IN-46 is a potent and orally active Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.082 μM. LSD1-IN-46 interrupts the β-catenin-mediated transcriptional program, thereby suppressing the stemness of gastric cancer cells. LSD1-IN-46 exhibits strong anti-tumor activity. LSD1-IN-46 can be used for the research of gastric 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。
- CAS 番号: 2982716-97-0
- 分子式: C22H29N3O
- 分子量:351.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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LSD1 0.082 μM (IC50) |
LSD1-IN-46 (Compound X-1) (0.5-2 μM; 5 days) increases H3K4me1/2 levels in MKN-45 cells and this effect is absent in LSD1-KO cells[1].
LSD1-IN-46 (0.5-2 μM; 5 days) inhibits self-renewal, sphere formation and colony formation of MKN-45 cells, and downregulates the expression of β-catenin, c-Myc and stemness markers OCT4, NANOG, SOX2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN-45
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Concentration:0.5, 1, 2 μM
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Incubation Time:5 days
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Result:Decreased OCT4, NANOG, and SOX2 levles.
Downregulated the expression of β-catenin, c-Myc.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice with injection of MFC gastric cancer cells (male, 6-8 weeks old)[1]
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Dosage:10, 20 mg/kg
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Administration:Oral gavage; Once daily; 11 days
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Result:Reduced tumor size and weight.
Did not affect mouse body weight or causing obvious hepatorenal toxicity.
Downregulated the expression of β-catenin, c-Myc, SOX2, NANOG in tumor tissues.
化学情報
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CAS 番号 2982716-97-0
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分子量 351.49
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分子式 C22H29N3O
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SMILES
CN(C)C(CC1)CCN1CCCN2C3=C(C=CC=C3)OC4=CC=CC=C24
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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)