2. Immunology/Inflammation Epigenetics Cell Cycle/DNA Damage Cytoskeleton Neuronal Signaling
  3. COX HDAC Microtubule/Tubulin Interleukin Related Amyloid-β Tau Protein
  4. COX-2/HDAC6-IN-1

COX-2/HDAC6-IN-1 (Compound 11e) 是一种双重 COX-2 和 HDAC6 抑制剂，其 HDAC6 IC50 为 0.12 μM，COX-2 IC50 为 0.66 μM。COX-2/HDAC6-IN-1 可增强 α-tubulin 乙酰化水平，调控表观遗传基因表达，抑制促炎介质 (COX-2、IL-1β、IL-6 和 TNF-α) 的表达。COX-2/HDAC6-IN-1 可促进 Amyloid-β 清除，减少 Tau 蛋白过度磷酸化。COX-2/HDAC6-IN-1 可通过稳定 MAP2 维持神经元形态，通过调节突触素保护突触完整性，恢复记忆相关基因的表达。COX-2/HDAC6-IN-1 具有神经保护活性，可在 Scopolamine (HY-N0296) 诱导的阿尔茨海默病小鼠模型中改善学习与记忆能力。COX-2/HDAC6-IN-1 可用于阿尔茨海默病的相关研究。

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COX-2/HDAC6-IN-1

COX-2/HDAC6-IN-1 Chemical Structure

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COX-2/HDAC6-IN-1 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

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 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC50 of 0.12 μM against HDAC6 and an IC50 of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease[1].

IC50 & Target[1]

HDAC6

0.12 μM (IC50)

COX-2

0.66 μM (IC50)

IL-6

 

IL-1β

 

体外研究
(In Vitro)

COX-2/HDAC6-IN-1 可强效抑制 HDAC6 (IC50 = 0.12 μM) 和 COX-2 (IC50 = 0.66 μM)[1]。

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

COX-2/HDAC6-IN-1 相关抗体:
体内研究
(In Vivo)

COX-2/HDAC6-IN-1 (1 mg/kg/天；腹腔注射；14 天) 在 Scopolamine (HY-N0296) 诱导的阿尔茨海默病小鼠模型中改善学习和记忆能力[1]。

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

Animal Model: albino mice (male, 8-10 weeks old, 30-35 g, scopolamine-induced AD model)[1]
Dosage: 1 mg/kg/day
Administration: i.p.; 14 days
Result: Produced a 4.3-fold increase in spontaneous alternation percentage in the Y-maze test compared to the scopolamine-induced AD group, and a 2.2-fold and 3.6-fold increase compared to the compound 10a and 11a groups, respectively.
Reduced the time to reach the ground in the pole climbing test by 42.3% compared to the scopolamine-induced AD group, with times 27% and 11.4% lower than the compound 10a and 11a groups, respectively.
Decreased GFAP gene expression by 54.7% (to 1.019 ± 0.05 RCN) compared to the scopolamine-induced AD group.
Increased MAP2 gene expression by 46.5% (to 0.747 ± 0.03 RCN) compared to the scopolamine-induced AD group.
Increased synaptophysin gene expression by 39.2% (to 0.891 ± 0.08 RCN) compared to the scopolamine-induced AD group.
Reduced Aβ1-40 concentration to 19.71 ± 2.13 pg/mg protein (62.41% decrease) compared to the scopolamine-induced AD group.
Reduced IL-1β concentration to 1.8 ± 0.4 pg/mg protein (71.8% decrease) compared to the scopolamine-induced AD group.
Reduced IL-6 concentration to 6.96 ± 1.55 pg/mg protein (67.7% decrease) compared to the scopolamine-induced AD group.
Reduced TNF-α concentration to 59.55 ± 3.17 ng/mg protein (65.07% decrease) compared to the scopolamine-induced AD group.
Increased acetylated histone H3 protein expression by 2-fold (to 0.7 ± 0.04 pg/mg protein) compared to the scopolamine-induced AD group.
Increased acetylated α-tubulin protein expression by 3.03-fold (to 1 ± 0.048 pg/mg protein) compared to the scopolamine-induced AD group.
Reduced COX-2 protein expression by 33.5% (to 0.355 ± 0.02 pg/mg protein) compared to the scopolamine-induced AD group.
Reduced MDA levels by 75% (to 1.3 ± 0.08 nmol/mg protein) compared to the scopolamine-induced AD group.
Increased GSH levels by 2.05-fold (to 7 ± 0.31 nmol/mg protein) compared to the scopolamine-induced AD group.
Reduced NO concentration by 83.2% (to 1.98 ± 0.23 μmol/mg protein) compared to the scopolamine-induced AD group.
Restored semi-normal histoarchitecture of the cerebral cortex with minimal pyknotic nuclei and pericellular edema; increased pyramidal cell counts and reduced total histopathologic scoring compared to the scopolamine-induced AD group.
Reduced insoluble Aβ plaque staining to 0.346 ± 0.108 compared to the scopolamine-induced AD group.
Reduced phosphorylated Tau immunoreactivity to 0.277 ± 0.066 (nearly normal levels) compared to the scopolamine-induced AD group.
Reduced phosphorylated STAT3 (705) expression to mild levels compared to the scopolamine-induced AD group.
分子量

487.53

Formula

C23H25N3O7S
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

COX-2/HDAC6-IN-1 相关分类

  • 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.

Keywords:

COX-2/HDAC6-IN-1COXHDACMicrotubule/TubulinInterleukin RelatedAmyloid-βTau ProteinCyclooxygenaseHistone deacetylasesILβ-amyloid peptideAβAbetaIL-1βHDAC6amyloid-βα-tubulinIL-6Alzheimer's diseaseTNF-αSTAT3COX-2TauInhibitorinhibitorinhibit

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