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

NB512 (compound 39a) 是 BETHDAC 的双效抑制剂,对 BRD4 溴结构域和 HDAC1/2 表现出高亲和力,EC50s 值为 100-400 nM。NB512 在癌细胞 PaTu8988T 和 NMC 中具有抗增殖活性。

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NB512 Chemical Structure

NB512 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

NB512 (1 μM) 抑制组蛋白 H3 K9/K14 脱乙酰化,以剂量依赖的方式上调 BET 靶向标记物 HEXIM1 和细胞周期调节基因 p57 在 PaTu8988T 中的表达[1]
NB512 (1 μM) 在 PaTu8988T 和 NMC 中表现出抗增殖活性,IC50 为 3.6 和 0.42 μM[1]
NB512 (1 μM) 下调致癌转录因子 MYC 和 TP63 在 NMC 细胞中的表达[1]

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

Formula

C26H21N5O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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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NB512
目录号:
HY-163282
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