1. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  2. HDAC Apoptosis PERK Microtubule/Tubulin
  3. HDAC6-IN-74

HDAC6-IN-74 是一种口服有效的选择性组蛋白去乙酰化酶 6 (HDAC6) 抑制剂,IC50 为 0.036 μM。HDAC6-IN-74 可诱导肿瘤细胞凋亡 (apoptosis),将细胞阻滞于细胞周期的 S 期,并减弱细胞的迁移、侵袭和克隆形成能力。HDAC6-IN-74 具有抗癌作用且无明显毒性。HDAC6-IN-74 可用于肝癌等癌症的研究。

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HDAC6-IN-74

HDAC6-IN-74 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer[1].

IC50 & Target[1]

HDAC6

0.036 μM (IC50)

HDAC1

3.0 μM (IC50)

HDAC2

2.3 μM (IC50)

HDAC3

4.9 μM (IC50)

HDAC4

2.1 μM (IC50)

HDAC5

8.4 μM (IC50)

HDAC10

1.7 μM (IC50)

HDAC11

6.4 μM (IC50)

体外研究
(In Vitro)

HDAC6-IN-74 (compound 14a) (0.05-50.0 μM; 72 h) 可强效抑制 HepG2 肝癌细胞的增殖,其 IC50 为 0.7 μM,对 Huh7 细胞的活性较低,对 LM3 细胞无活性,且相对于非致瘤细胞系,对肿瘤细胞具有高选择性[1]
HDAC6-IN-74 (1-10 μM; 0-72 h) 可诱导 HepG2 细胞发生凋亡和 S 期细胞周期阻滞,抑制细胞侵袭和迁移[1]
HDAC6-IN-74 (0-10.0 μM; 24 h) 可在 HepG2 细胞中下调 HDAC6 与 p-ERK1/2 的表达,并上调 Ac-H3 与 Ac-α-tubulin 的表达[1]

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

Cell Proliferation Assay[1]

Cell Line: HepG2, Huh7, LM3, THLE-2
Concentration: 50.0, 25.0, 10.0, 5.0, 2.5, 1.0, 0.5, 0.1 and 0.05 μM
Incubation Time: 72 h
Result: Exhibited an IC50 of 0.7 μM against HepG2 cells, 9.4 μM against Huh7 cells, >50 μM against LM3 cells, >50 μM against THLE-2 cells.

Apoptosis Analysis[1]

Cell Line: HepG2
Concentration: 1 μM, 10 μM
Incubation Time: 72 h
Result: Induced an apoptotic rate of 19.48% at 1 μM.
Induced an apoptotic rate of 25.73% at 10 μM.

Western Blot Analysis[1]

Cell Line: HepG2
Concentration: 0, 0.5, 1.0, 2.5, 5.0 and 10.0 μM
Incubation Time: 24 h
Result: Significantly reduced HDAC6 and p-ERK1/2 protein levels at 2.5 μM.
Dose-dependently increased Ac-H3 and Ac-α-tubulin protein levels without affecting total H3 or α-tubulin levels at concentrations from 0.5 to 10.0 μM.
体内研究
(In Vivo)

HDAC6-IN-74 (12.5-25.0 mg/kg; 灌胃; 隔日一次; 24 天) 对 HepG2 异种移植瘤展现出强效的剂量依赖性体内抗肿瘤活性[1]

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

Animal Model: BALB/c nude mice treated HepG2 (female, 6-week-old)[1]
Dosage: 12.5 mg/kg; 25.0 mg/kg
Administration: Intragastric administration.; every other day; 24 days
Result: Achieved a 47.6% tumor inhibition rate, significantly reduced HDAC6 protein levels in tumor tissue, significantly increased Ac-α-tubulin protein levels in tumor tissue, and induced tumor cell apoptosis at 12.5 mg/kg.
Achieved a 90.2% tumor inhibition rate, caused a more significant reduction in HDAC6 protein levels in tumor tissue compared to the 12.5 mg/kg dose, increased Ac-α-tubulin protein levels to ~15.4-fold that of the control group, and induced the highest level of tumor cell apoptosis among the treatment groups at 25 mg/kg.
Caused no obvious changes in mouse body weight or histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney).
分子量

378.35

Formula

C16H17N3OSSe

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

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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:
HDAC6-IN-74
目录号:
HY-181579
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