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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- Formule: C26H21N5O2
- Masse moléculaire:435.48
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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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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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) |
In Vitro
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. Further protocols information, click here.
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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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Masse moléculaire 435.48
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Formule 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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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.
Protocole
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NB512 Related Classifications
HY-163282 Related Classifications
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