1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC Epigenetic Reader Domain
  3. 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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NB512

NB512 構造式

容量 在庫状況
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製品説明

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[1].

IC50 & Target

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)

体外実験

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.

Western Blot Analysis[1]

Cell Line: PaTu8988T
Concentration: 0-1 μM
Incubation Time: 48 h
Result: Increased acetylated histone H3 K9/K14 in a dose-dependent manner.

RT-PCR[1]

Cell Line: PaTu8988T
Concentration: 0-1 μM
Incubation Time: 6 h
Result: Upregulated mRNA levels of HEXIM1 and p57 in a dose-dependent manner.
分子量

435.48

分子式

C26H21N5O2

SMILES

O=C(NC1=CC(C2=CC=CC=C2)=CC=C1N)C3=NC=C(C4=CN(C)C(C5=C4C=CN5)=O)C=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
NB512
製品番号:
HY-163282
数量:
MCE 日本正規代理店: