1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC Histone Methyltransferase
  3. HDACs/EZH2-IN-1

HDACs/EZH2-IN-1 (Compound 22a) 是一种 HDACs/EZH2 抑制剂 (EZH2 Y641N 在 50 nM 时抑制率: 98%),其中对 HDAC1HDAC6 选择性抑制 (IC50分别为 0.23 μM 和 0.07 μM)。HDACs/EZH2-IN-1 抑制携带 EZH2 突变的弥漫性大 B 细胞淋巴瘤细胞和多种急性髓性白血病细胞的增殖。HDACs/EZH2-IN-1 具有诱导细胞分化和凋亡 (Apoptosis) 能力。

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HDACs/EZH2-IN-1 Chemical Structure

HDACs/EZH2-IN-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis[1].

IC50 & Target[1]

HDAC1

0.23 μM (IC50)

HDAC6

0.07 μM (IC50)

HDAC4

>10 μM (IC50)

HDAC11

>10 μM (IC50)

EZH2 WT

0.84 nM (IC50)

EZH2 Y641N

1.36 nM (IC50)

体外研究
(In Vitro)

HDACs/EZH2-IN-1 (5 μM, 48-120 h) 对携带 EZH2 Y641N 突变的 DLBCL 细胞 SU-DHL-6 具有强抗增殖效应,IC50 为 1.04 μM (48 h) 和 0.17 μM (120 h) [1]
HDACs/EZH2-IN-1 (0.1-100 μM, 48 h) 可抑制 AML 细胞的生长,IC50分别为 1.39 μM (MV4-11)、2.45 μM (U937) 和 1.32 μM (OCI-AML3)[1]
HDACs/EZH2-IN-1 (0.1-100 μM, 48 h) 可提高 HDAC1/2/3 的底物乙酰组蛋白 H3 (AC-HH3) 和 HDAC6 的底物乙酰-α-微管蛋白 (AC-α-tubulin) 的细胞内水平[1]
HDACs/EZH2-IN-1 (2 μM, 48 h) 可诱导 MOLM13 细胞分化,增加两种髓系成熟标志物 CD11b 和 CD14 的表达[1]
HDACs/EZH2-IN-1 (2-4 μM, 48 h) 诱导 MOLM13 细胞发生剂量依赖性凋亡[1]
HDACs/EZH2-IN-1 (1-2 μM) 协同抗 AML 药物 (阿糖胞苷 (HY-13605), 柔红霉素 (HY-13062A), 吉瑞替尼 (HY-12432)) 对 MOLM13 细胞发挥抗癌作用[1]
HDACs/EZH2-IN-1 在人体和大鼠血浆中具有良好的代谢稳定性,其 T1/2 分别大于 180 min 和 138 min[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SU-DHL-6, MOLM-13, OCI-AML2, MV4-11, U937 and OCI-AML3
Concentration: 0.1, 1, 5, 10, 100 μM
Incubation Time: 48, 120 h
Result: Displayed strong antiproliferative activities against SU-DHL-6 cells (5 μM, 48 h and 120 h).
Inhibited the growth of cell lines, with IC50 of 1.39 μM (MV4-11), 2.45 μM (U937), and 1.32 μM (OCI-AML3) (1, 10, 100 μM, 48 h).

Western Blot Analysis[1]

Cell Line: MOLM13 cells
Concentration: 4 μM
Incubation Time: 6 h
Result: Increased the intracellular levels of the HDAC1/2/3 substrate acetylhistone H3 (AC-HH3) and the HDAC6 substrate acetyl-α-tubulin (AC-α-tubulin).
Led to a significant reduction in the levels of trimethylation at H3K27.
分子量

626.54

Formula

C29H36BrN7O4

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
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  • 稀释计算器

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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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产品名称:
HDACs/EZH2-IN-1
目录号:
HY-169400
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