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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
-
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
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.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LSD1-IN-46 Related Classifications
HY-179339 Related Classifications
Powered by Bioz