2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC6-IN-69

HDAC6-IN-69 是一种可透过血脑屏障、高选择性的 HDAC6 抑制剂，其 IC50 为 4.0 nM，对其他 HDAC 亚型的选择性超过 176 倍。HDAC6-IN-69 能在神经元细胞中剂量依赖性地上调乙酰化 α-微管蛋白水平，从而发挥神经保护作用，可用于缺血性中风研究。

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HDAC6-IN-69

HDAC6-IN-69 Chemical Structure

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Customer Review

HDAC6-IN-69 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

HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research [1].

IC50 & Target[1]

HDAC1

1135 nM (IC50)

HDAC3

9.0 nM (IC50)

HDAC4

1248 nM (IC50)

HDAC6

4.0 nM (IC50)

HDAC8

702.5 nM (IC50)

HDAC11

1243.0 nM (IC50)

体外研究
(In Vitro)

HDAC6-IN-69 (compound 8k) 具有良好的药代动力学特征，在人及大鼠肝微粒体中均表现出中等清除率和代谢稳定性 (人肝微粒体半衰期T1/2 = 154.00 min，大鼠肝微粒体半衰期T1/2 = 29.49 min)，且心脏毒性风险较低[1]。
HDAC6-IN-69 (1.0-10 μM，处理 24 小时) 能在人神经母细胞瘤细胞 (SH-SY5Y 细胞) 中选择性抑制 HDAC6 而非 HDAC1[1]。
HDAC6-IN-69 (0.1-10 μM，预处理 0.5 小时) 在 L-glutamate (HY-N0455B) 诱导的 SH-SY5Y 细胞损伤模型中具有潜在的神经保护活性[1]。

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

HDAC6-IN-69 相关抗体:

Cell Viability Assay[1]

Cell Line: Human neuroblastoma cells
Concentration: 0.1 μM,1 μM,10 μM
Incubation Time: 24 h
Result: Efficiently transported to SH-SY5Y cells and upregulated the expression of acetylated α-tubulin in a dose-dependent manner, while the expression of acetylated histone H3 was only moderately affected

Cell Cytotoxicity Assay[1]

Cell Line: L-glutamate induced-SH-SY5Y cells
Concentration: 0.1 μM,1 μM,10 μM
Incubation Time: 0.5 h
Result: Increased the survival rate of damaged cells at low and medium doses
Exhibit more stable neuroprotective activity and a wide therapeutic range
Showed a downward trend at high concentrations
Showed a high cell survival rate at high concentrations
体内研究
(In Vivo)

HDAC6-IN-69 (compound 8k) (6 或 12.5 mg/kg，静脉注射，单次给药) 在大脑中动脉闭塞大鼠模型中显示出缓解中风所致脑梗死的巨大潜力[1]。

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

Animal Model: Ischemia induced (a nylon thread was gently inserted from the common carotid artery into the middle cerebral artery for 1.5 hours)-male Sprague-Dawley (SD) rats (240 g)[1].
Dosage: 6 or 12.5 mg/kg
Administration: i.v., once
Result: Reduced the cerebral infarction area (from 32.87% to 13.13%).
分子量

425.30

Formula

C17H17BrN2O4S
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

HDAC6-IN-69 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)

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.

Keywords:

HDAC6-IN-69HDACHistone deacetylasesHDAC6Neuroprotective Agentα-tubulinischemic strokeInhibitorinhibitorinhibit

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产品名称：
HDAC6-IN-69
目录号：
HY-180214
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