2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Apoptosis Caspase
  4. HDAC-IN-94

HDAC-IN-94 是一种强效、选择性的 HDAC6 抑制剂 (IC50 = 4.5 nM)。HDAC-IN-94 对 HDAC6 的选择性是对 HDAC8 的 1000 倍以上，并且对其他亚型 (HDAC1-3/10) 的活性极弱。HDAC-IN-94 诱导 α- 微管蛋白 (α-tubulin) 的超乙酰化、细胞凋亡 (apoptosis) 和 G2/M 期细胞周期阻滞，有强大对抗肿瘤功效和较低的细胞毒性。HDAC-IN-94 可用于神经母细胞瘤和胶质母细胞瘤的相关研究。

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HDAC-IN-94

HDAC-IN-94 Chemical Structure

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HDAC-IN-94 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

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research[1].

IC50 & Target[1]

hHDAC6

4.5 nM (IC50)

hHDAC8

3273 nM (IC50)

hHDAC1

403 nM (IC50)

hHDAC10

202 nM (IC50)

hHDAC2

537 nM (IC50)

hHDAC3

1278 nM (IC50)

hHDAC5

4455 nM (IC50)

hHDAC11

>10000 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-94 (compound 5o) 能够嵌入 hHDAC6 的催化位点，其中以中性形式模拟的羟肟酸基团能够螯合锌原子，其极性苯甲酰胺上的氢原子与 Ser568 形成氢键[1]。
HDAC-IN-94 (1-10 μM，24 小时) 在 SH-SY5Y 细胞中以剂量依赖性的方式促进 α- 微管蛋白的乙酰化[1]。
HDAC-IN-94 (10 nM-30 μM，24-72 小时) 在浓度高达 30 μM 时，对 HEK-293 细胞未显示出细胞毒性[1]。
HDAC-IN-94 (24-72 小时) 对 U87-MG、T98G、U251-MG 和 SH-SY5Y 细胞表现出抗增殖活性，其 IC50 值分别为 51.31、42.60、2.37 和 3.32 μM[1]。
HDAC-IN-94 (3 μM，24 小时) 在 SH-SY5Y 细胞中能促进 G2/M 期细胞周期阻滞、触发程序性细胞死亡，并引起轻微的自噬 (autophagy) 刺激[1]。
HDAC-IN-94 (3-30 μM，24-72 小时) 在 SH-SY5Y 细胞中表现出明确的时间和浓度依赖性的促凋亡活性[1]。

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

HDAC-IN-94 相关抗体:

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 1 and 10 μM
Incubation Time: 24 h
Result: Promoted acetylation of α-tubulin in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Led to an accumulation of hypodiploid SH-SY5Y cells in the subG0/G1 phase.
Showed a decrease in the G0/G1 population and a slight increase in cells within the S-phase.

Apoptosis Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 3, 10, and 30 μM
Incubation Time: 24, 48 and 72 h
Result: Induced a concentration-dependent increase in early apoptosis at 24 h.
Induced a significant increase of late apoptosis starting at 10 μM (24 h).
Showed significant effects on both early and late apoptosis at 10 μM and a pronounced apoptotic response at 30 μM (46 % for early and 27 % for late apoptosis), at 48 h of treatment.
Significantly increased early and late apoptosis at all concentrations at 72 h.
Induced a concentration-dependent increase in caspase-3/7 activation, starting from 10 μM at 24 h.
Elicited 24% caspase-positive cells at 30 μM at 24 h.
Showed a significant increase in caspase activation at 10 μM and 30 μM at 48 h.
Continued to activate caspase-3/7 in a concentration-dependent manner after 72 h, with 43 % positivity at 30 μM.
分子量

342.35

Formula

C18H18N2O5
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

HDAC-IN-94 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:

HDAC-IN-94HDACMicrotubule/TubulinApoptosisCaspaseHistone deacetylasesHDAC6α-tubulinneuroblastomaglioblastomaU87-MGT98GU251-MGSH-SY5YInhibitorinhibitorinhibit

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产品名称：
HDAC-IN-94
目录号：
HY-179019
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