NB512
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC.
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- Fòrmula: C26H21N5O2
- Peso molecular:435.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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HDAC2 0.1 μM (EC50) |
HDAC1 0.11 μM (EC50) |
BRD4 BD2 0.25 μM (EC50) |
BRD4 BD1 0.36 μM (EC50) |
HDAC3 13.6 μM (EC50) |
NB512 (1 μM) inihibits the deacetylation of histone H3 K9/K14, upregulates the BET targeting marker HEXIM1 and cell cycle regulator gene p57 in PaTu8988T in a dose-dependent manner[1].
NB512 (1 μM) exhibits an anti-proliferative activity towards PaTu8988T and NMC, with IC50s of 3.6 and 0.42 μM, respectively[1].
NB512 (1 μM) downregulates oncogenic transcription factors MYC and TP63 in NMC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PaTu8988T
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Concentration:0-1 μM
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Incubation Time:48 h
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Result:Increased acetylated histone H3 K9/K14 in a dose-dependent manner.
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Cell Line:PaTu8988T
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Concentration:0-1 μM
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Incubation Time:6 h
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Result:Upregulated mRNA levels of HEXIM1 and p57 in a dose-dependent manner.
Chemical Information
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Peso molecular 435.48
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Fòrmula C26H21N5O2
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SMILES
O=C(NC1=CC(C2=CC=CC=C2)=CC=C1N)C3=NC=C(C4=CN(C)C(C5=C4C=CN5)=O)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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