1. Epigenetics
  2. Histone Demethylase
  3. 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.

For research use only. We do not sell to patients.

LSD1-IN-46

LSD1-IN-46 Chemical Structure

CAS No. : 2982716-97-0

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Description

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[1].

IC50 & Target[1]

LSD1

0.082 μM (IC50)

In Vitro

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.

Western Blot Analysis[1]

Cell Line: MKN-45
Concentration: 0.5, 1, 2 μM
Incubation Time: 5 days
Result: Decreased OCT4, NANOG, and SOX2 levles.
Downregulated the expression of β-catenin, c-Myc.
In Vivo

LSD1-IN-46 (Compound X-1) (10-20 mg/kg; i.g.; Once daily; once daily for 11 days) reduces tumor size and weight in subcutaneous injection of MFC gastric cancer cells in BALB/c nude[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice with injection of MFC gastric cancer cells (male, 6-8 weeks old)[1]
Dosage: 10, 20 mg/kg
Administration: Oral gavage; Once daily; 11 days
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.
Molecular Weight

351.49

Formula

C22H29N3O

CAS No.
SMILES

CN(C)C(CC1)CCN1CCCN2C3=C(C=CC=C3)OC4=CC=CC=C24

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LSD1-IN-46
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HY-179339
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