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.
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- CAS. Nr.: 2982716-97-0
- Formel: C22H29N3O
- Molecular Weight:351.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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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.
Chemical Information
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CAS. Nr. 2982716-97-0
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Molecular Weight 351.49
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Formel C22H29N3O
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SMILES
CN(C)C(CC1)CCN1CCCN2C3=C(C=CC=C3)OC4=CC=CC=C24
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LSD1-IN-46 Related Classifications
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