2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. ZWZH-21

WZH-21 是一种选择性且具有口服活性的 HDAC1/2 双重抑制剂，对 HDAC1 的 IC50 值为 34 nM，对 HDAC2 的值为 41 nM。ZWZH-21 能够抑制 HCT116 和 SW480 细胞的生长，IC50 值分别为 0.524 μM 和 1.063 μM。ZWZH-21 可以抑制多种结直肠癌细胞的增殖和迁移，并诱导其凋亡 (apoptosis)。ZWZH-21 可用于癌症研究，如结直肠癌研究。

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ZWZH-21

ZWZH-21 Chemical Structure

CAS No. : 3069195-42-9

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ZWZH-21 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer[1].

IC50 & Target[1]

HDAC1

34 nM (IC50)

HDAC2

41 nM (IC50)

HDAC3

277 nM (IC50)

HDAC6

>800 nM (IC50)

HDAC8

>800 (IC50)

体外研究
(In Vitro)

ZWZH-21 可抑制 A549、MCF-7 和 HepG2 细胞的生长，其 IC50 值分别为 1.66 μM、2.445 μM 和 1.551 μM[1]。
ZWZH-21 (0.4-1.6 μM, 48 h) 可抑制 HCT116 细胞中温度诱导的 HDAC1/2 降解[1]。
ZWZH-21 (0.4-1.6 μM, 48 h) 在 HCT116 细胞中以浓度依赖的方式诱导 HDAC1 和 HDAC2 蛋白的降解，以及 Ac-H3 和组蛋白 H4 的形成[1]。
ZWZH-21 (0.4-1.6 μM, 48 h) 可抑制 HCT116 和 SW480 细胞的集落形成能力[1]。
ZWZH-21 (0.4-2 μM, 48 h) 可抑制 HCT116 和 SW480 细胞的迁移并诱导其凋亡[1]。
ZWZH-21 (0.4-2 μM, 48 h) 可诱导 HCT116 和 SW480 细胞发生 G1 期阻滞[1]。

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

ZWZH-21 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.4, 0.8, and 1.6 μM
Incubation Time: 48 h
Result: Reduced HDAC1 and HDAC2 protein and increased Ac–H3 and Ac–H4 levels.

Apoptosis Analysis[1]

Cell Line: HCT116 cells and SW480 cells
Concentration: 0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
Incubation Time: 48 h
Result: Significantly increased the proportion of Annexin V-positive cells.
Showed highest apoptotic rates reaching 60.7 % and 40.04 % at low concentrations.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells and SW480 cells
Concentration: 0.4, 0.8 and 1.6 μM in HCT116, 0.5, 1 and 2 μM in SW480 cells
Incubation Time: 24 h
Result: Demonstrated a dose-dependent accumulation of cells in G1 phase.
体内研究
(In Vivo)

ZWZH-21 (2000 mg/kg，口服一次) 在小鼠中显示出良好的安全性[1]。
ZWZH-21 (30-120 mg/kg，灌胃， 每天一次，持续 14 天) 可抑制携带 HCT116 人结肠癌异种移植物的小鼠的肿瘤生长[1]。

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

Animal Model: Mice bearing HCT116 human colon cancer xenografts[1]
Dosage: 30, 60 and 120 mg/kg
Administration: Oral gavage, daily for 14 days
Result: Showed no significant body weight changes.
Suppressed tumor growth.
分子量

422.48

Formula

C26H22N4O2
CAS 号
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

ZWZH-21 相关分类

  • 摩尔计算器

  • 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.

Keywords:

ZWZH-213069195-42-9ZWZH21ZWZH 21HDACApoptosisHistone deacetylasesHDAC1HDAC2HCT116SW480Colorectal cancerInhibitorinhibitorinhibit

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