N-Myc-IN-1
N-Myc-IN-1 is a selective N-Myc inhibitor/degrader with a Kd value of 1.47 μM. N-Myc-IN-1 promotes phosphorylation of N-Myc at threonine-58, triggers N-Myc degradation via the ubiquitin-proteasome pathway, and suppresses the expression of N-Myc target genes. N-Myc-IN-1 reduces the viability of MYCN-dependent tumor cells and induces apoptosis. N-Myc-IN-1 can be used in the research of neuroblastoma.
For research use only. We do not sell to patients.
- CAS No.: 885986-52-7
- Formula: C15H13BrN4O2
- Molecular Weight:361.19
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SK-N-BE(2), IMR-32, NB1 cells
-
Concentration:2, 4 and 8 μM
-
Incubation Time:48 h
-
Result:Induced cell apoptosis.
-
Cell Line:SK-N-BE(2), IMR-32, NB1 cells
-
Concentration:1, 2, 4 and 8 μM
-
Incubation Time:12 h
-
Result:Increased cleaved-PARP and decreased BCL-XL.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c-nude (male, 6-8-week-old, subcutaneous xenograft model)[1]
-
Dosage:10 mg/kg; 20 mg/kg
-
Administration:i.p.; once daily for 18 days
-
Result:Achieved a tumor growth inhibition (TGI) value of 79.4%.
Achieved a tumor growth inhibition (TGI) value of 61.4%.
Significantly reduced tumor weights compared to controls.
Decreased Ki67 and N-Myc levels in tumor tissues.
Increased phosphorylation of N-Myc at threonine 58 in tumor tissues.
Was well-tolerated, with no significant mouse body weight loss or apparent toxicity in major organs.
- Kinase activity and phosphorylation assays
- Western Blot
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
-
CAS No. 885986-52-7
-
Molecular Weight 361.19
-
Formula C15H13BrN4O2
-
SMILES
O=C(CBr)NC1=CC2=NN(C3=CC=C(C=C3)OC)N=C2C=C1
-
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)