2. Apoptosis Epigenetics Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Apoptosis HDAC Microtubule/Tubulin Reactive Oxygen Species
  4. Tubulin/HDAC-IN-4

Tubulin/HDAC-IN-4 (compound 9n) 是一种微管 (Tubulin) 和 HDAC 双重抑制剂，对 HDAC1、HDAC2、HDAC6、HDAC7 的 IC50 值分别为 0.73、0.43、0.62、2.34 µM。Tubulin/HDAC-IN-4 通过靶向秋水仙碱结合位点抑制微管蛋白聚合。Tubulin/HDAC-IN-4 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期。Tubulin/HDAC-IN-4 诱导细胞内 ROS 水平显着升高。Tubulin/HDAC-IN-4 显示出抗血管生成活性和抗癌活性。

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Tubulin/HDAC-IN-4 Chemical Structure

Tubulin/HDAC-IN-4 Chemical Structure

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Tubulin/HDAC-IN-4 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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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

Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity[1].

IC50 & Target[1]

HDAC1

0.73 μM (IC50)

HDAC2

0.43 μM (IC50)

HDAC6

0.62 μM (IC50)

HDAC7

2.34 μM (IC50)

体外研究
(In Vitro)

Tubulin/HDAC-IN-4 (compound 9n) (0-10 µM; 72 h) 对 MDA-MB-231、A549 表现出细胞毒性，IC50s 为 0.34、0.29、0.016、0.15、0.16 µM 分别为 PC-3、U251、MCF-7 细胞[1]。
Tubulin/HDAC-IN-4（2.5、5、10、20、40 nM；24 小时）以剂量依赖性方式抑制 PC-3 细胞集落形成[1]。
Tubulin/HDAC-IN-4 (0.2、1、5、25 µM) 抑制微管蛋白聚合，IC50值为 4.82 µM[1]。
Tubulin/HDAC-IN-4（0.08、0.16、0.32；24 h）可增加 PC-3 细胞中 Ac-α-tubulin 和 Ac-Histone H3 的表达[1]。
Tubulin/HDAC-IN-4（0.08、0.16、0.32 µM；24 小时）诱导细胞凋亡和 G2/M 期细胞周期停滞[1]。
Tubulin/HDAC-IN-4（0.08、0.16、0.32 µM；24 小时）可诱导细胞内 ROS 水平显着升高[1]。

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

Tubulin/HDAC-IN-4 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231, A549, PC-3, U251, MCF-7 cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed cytotoxicity with IC50s of 0.34, 0.29, 0.016, 0.15, 0.16 µM for MDA-MB-231, A549, PC-3, U251, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Increased in both the expression of HDAC6 substrate Ac-α-tubulin and HDAC1/2/3 substrate Ac-Histone H3 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Dose-dependently arrested PC-3 cells at G2/M phase, decreased in expression level of p-Cdc25cSer216, p-Cdc2Thr216 and p-CdcTyr15, increased the expression of Cyclin B1.

Apoptosis Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Induced apoptosis and increased the expression of cleaved PARP and cleaved Caspase 3, decreased the expression of Bim and Bcl-2.
体内研究
(In Vivo)

Tubulin/HDAC-IN-4 (10, 20 mg/kg; i.v.; every two days for 21 days) 显示出抗癌活性[1]。

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

Animal Model: 5-week-old male BALB/c nude mouse (PC-3 cells)[1]
Dosage: 10, 20 mg/kg
Administration: I.v.; every two days for 21 days
Result: Inhibited the growth of tumor with the tumor growth inhibition (TGI) reached 90.07% at 20 mg/kg.
分子量

438.47

Formula

C24H26N2O6
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

Tubulin/HDAC-IN-4 相关分类

  • 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)

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The dilution calculator equation

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

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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.

Keywords:

Tubulin/HDAC-IN-4ApoptosisHDACMicrotubule/TubulinReactive Oxygen SpeciesHistone deacetylasesapoptosisROS levelsG2/MPC-3 cellsInhibitorinhibitorinhibit

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