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.
- CAS No.: 2982716-97-0
- Formula: C22H29N3O
- Molecular Weight:351.49
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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.
-
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.
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.
Chemical Information
-
CAS No. 2982716-97-0
-
Molecular Weight 351.49
-
Formula C22H29N3O
-
SMILES
CN(C)C(CC1)CCN1CCCN2C3=C(C=CC=C3)OC4=CC=CC=C24
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)