2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis Others
  3. HDAC Reactive Oxygen Species (ROS) Apoptosis Necroptosis Biochemical Assay Reagents Caspase Bcl-2 Family
  4. HDAC8-IN-14

HDAC8-IN-14 是一种姜黄素衍生物，是一种选择性 HDAC8 抑制剂，Ki 值为 9 nM。HDAC8-IN-14 可诱导活性氧 (ROS) 的产生，破坏线粒体膜电位，并促进细胞凋亡 (apoptosis)。HDAC8-IN-14 可显著促进细胞在亚 G0/G1 期积累，这与细胞凋亡 (apoptosis) 或坏死 (necroptosis) 相符。HDAC8-IN-14 可诱导细胞色素 c (cytochrome c)、裂解型 caspase-3 和促凋亡蛋白 Bak 的表达上调，而抗凋亡蛋白 Bcl-2 的水平保持不变。HDAC8-IN-14 可用于白血病的研究。

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HDAC8-IN-14

HDAC8-IN-14 Chemical Structure

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Customer Review

HDAC8-IN-14 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

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia[1].

IC50 & Target

HDAC8

9 nM (Ki)

Caspase-3

 

体外研究
(In Vitro)

HDAC8-IN-14 (Compound 5e) (0.1-100 μM，48 小时) 在 MOLT-4 细胞中表现出较低的值 (IC50 = 90 nM)，在 EL-4 细胞中 IC50 值为 1.98 μM，在 YAC-1 细胞中为 1.17 μM，在 L1210 细胞中为 18.94 μM，而在非癌性 HEK-293 细胞系中则表现出显著更高的值 (IC50 = 39.20 μM) ，表明其在有效浓度下对非癌细胞具有选择性和安全性[1]。
HDAC8-IN-14 (100 nM，30 分钟) 在 MOLT-4 细胞中显示出显著的 ROS 诱导作用，该作用通过荧光染料 H2DCFDA (HY-D0940) 进行检测[1]。
HDAC8-IN-14 (48 小时) 可诱导线粒体去极化，表现为 JC-1 荧光强度的变化；可触发细胞凋亡 (约 10%) 和坏死 (约 30%) ；并导致细胞周期阻滞，其特征是亚 G0 期凋亡细胞比例增加 20%，同时 G0/G1 期和 G2/M 期细胞比例减少，S 期细胞比例略有增加[1]。
HDAC8-IN-14 (50-100 nM，48 小时) 可显著上调细胞色素 c、裂解型 caspase-3 和促凋亡蛋白 Bak 的表达，而抗凋亡蛋白 Bcl-2 的水平保持不变，表明其在 MOLT-4 细胞中通过一种不依赖于 Bcl-2 的机制激活内源性凋亡途径[1]。

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

HDAC8-IN-14 相关抗体:

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 50 nM, 100 nM
Incubation Time: 48 h
Result: Induced a significant upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered.
体内研究
(In Vivo)

HDAC8-IN-14 (50 mg/kg，腹腔注射，每日一次，持续 30 天) 能有效抑制 DLA 小鼠模型中的肿瘤生长，且不表现出明显的全身毒性[1]。

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

Animal Model: The left thigh of each female Swiss albino mice (6-8 weeks) was injected with 0.5 million DLA cells to induce a tumor[1].
Dosage: 50 mg/kg
Administration: I.p., once daily for 30 days
Result: Reduced tumor burden compared to the control group.
Resulted in the upregulation of cytochrome c, cleaved caspase 3, and proapoptotic Bax, the levels of the anti-apoptotic Bcl-2 remained unchanged.
Exhibited reduced nuclear density, suggesting decreased tumor cell proliferation.
No significant histopathological alterations were observed in the liver and kidney tissues of treated mice.
Indicated no toxicity to liver function.
The body weight of the animals at the end of the study showed no variation.
分子量

628.55

Formula

C37H27Cl2N5O
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

HDAC8-IN-14 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:

HDAC8-IN-14HDACReactive Oxygen Species (ROS)ApoptosisNecroptosisBiochemical Assay ReagentsCaspaseBcl-2 FamilyHistone deacetylasesCurcuminoidCurcuminoid analoguesCytotoxicityDockingLeukemiaPiperidone derivativesInhibitorinhibitorinhibit

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