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.
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- CAS No.: 885986-52-7
- Formule: C15H13BrN4O2
- Masse moléculaire:361.19
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
N-Myc-IN-1 (Compound N78) (72 h) significantly inhibits the viability of N-Myc high-expressing cells such as SK-N-BE (2) and IMR-32[1].
N-Myc-IN-1 (1-8 μM; 8-48 h) induces apoptosis in SK-N-BE (2), IMR-32 and NB1 cells via degradation of N-Myc[1].
N-Myc-IN-1 (0-8 μM) promotes GSK3β-mediated phosphorylation of T58 to target N-Myc for ubiquitin-proteasomal degradation, rather than through the lysosomal pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-BE(2), IMR-32, NB1 cells
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Concentration:2, 4 and 8 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis.
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Cell Line:SK-N-BE(2), IMR-32, NB1 cells
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Concentration:1, 2, 4 and 8 μM
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Incubation Time:12 h
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Result:Increased cleaved-PARP and decreased BCL-XL.
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 (male, 6-8-week-old, subcutaneous xenograft model)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; once daily for 18 days
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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.
Chemical Information
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CAS No. 885986-52-7
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Masse moléculaire 361.19
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Formule C15H13BrN4O2
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SMILES
O=C(CBr)NC1=CC2=NN(C3=CC=C(C=C3)OC)N=C2C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
N-Myc-IN-1 Related Classifications
HY-186247 Related Classifications
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