COX-2/HDAC6-IN-1
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.
For research use only. We do not sell to patients.
- Formula: C23H25N3O7S
- Molecular Weight:487.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC6 0.12 μM (IC50) |
COX-2 0.66 μM (IC50) |
IL-6 |
IL-1β |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:albino mice (male, 8-10 weeks old, 30-35 g, scopolamine-induced AD model)[1]
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Dosage:1 mg/kg/day
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Administration:i.p.; 14 days
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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.
Chemical Information
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Molecular Weight 487.53
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Formula C23H25N3O7S
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SMILES
COC1=C(OC)C=CC(C2=CC(C(NCC(OCC)=O)=O)=NN2C3=CC=C(S(=O)(C)=O)C=C3)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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