HDAC2-IN-3
HDAC2-IN-3 is a selective, orally active, blood-brain barrier permeable HDAC2 inhibitor with an IC50 of 14 nM. HDAC2-IN-3 upregulates histone acetylation levels in cells and in vivo, and enhances long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 2652579-44-5
- Formula: C19H16N6OS
- Molecular Weight:376.43
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Description
IC50 & Target
[1]|
HDAC2 14 nM (IC50) |
In Vitro
HDAC2-IN-3 (Compound 11) (0.01-25.3 μM; 24 h) increases H4K12 acetylation in primary cortical neurons from C57B6J mouse embryos, with a maximum effect of 71% and an IC20 of 0.259 μM[1].
HDAC2-IN-3 (0.0411-83.3 μM; overnight) shows low activity against HDAC1 in HDAC2-KO K562 cells, with a maximum 12% increase in H3K9 acetylation relative to the positive control[1].
HDAC2-IN-3 (0.1-25 μM; 48 h) does not exhibit significant cytotoxicity toward human bone marrow CD34+ progenitor cells at concentrations up to 25 μM, with an IC50 > 25 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
HDAC2-IN-3 (50 mg/kg; p.o.; daily; 10 days) significantly enhances hippocampal LTP in 6- to 7-month-old APP/PS1 mice, indicating potential to improve learning and memory formation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APP/PS1 (male; transgenic model generated by crossing Tg2576 mice with heterozygous PSEN1I213T KI mice)[1]
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Dosage:50 mg/kg
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Administration:p.o.; single dose
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Result:Elevated hippocampal H4K12 acetylation levels to approximately 220% of vehicle-treated control levels.
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Animal Model:APP/PS1 (6- to 7-month-old; transgenic model generated by crossing Tg2576 mice with heterozygous PSEN1I213T KI mice)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 10 days
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Result:Significantly enhanced hippocampal LTP compared to vehicle-treated mice, with a statistically significant difference observed in the field excitatory postsynaptic potential slope following theta burst stimulation.
Chemical Information
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CAS No. 2652579-44-5
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Appearance Solid
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Molecular Weight 376.43
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Formula C19H16N6OS
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Color Light yellow to yellow
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SMILES
NC1=CC=C(C=C1NC(C2=CN=C(C=N2)C3=CN(N=C3)C)=O)C4=CC=CS4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (132.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6565 mL | 13.2827 mL | 26.5654 mL | 66.4134 mL |
| 5 mM | 0.5313 mL | 2.6565 mL | 5.3131 mL | 13.2827 mL | |
| 10 mM | 0.2657 mL | 1.3283 mL | 2.6565 mL | 6.6413 mL | |
| 15 mM | 0.1771 mL | 0.8855 mL | 1.7710 mL | 4.4276 mL | |
| 20 mM | 0.1328 mL | 0.6641 mL | 1.3283 mL | 3.3207 mL | |
| 25 mM | 0.1063 mL | 0.5313 mL | 1.0626 mL | 2.6565 mL | |
| 30 mM | 0.0886 mL | 0.4428 mL | 0.8855 mL | 2.2138 mL | |
| 40 mM | 0.0664 mL | 0.3321 mL | 0.6641 mL | 1.6603 mL | |
| 50 mM | 0.0531 mL | 0.2657 mL | 0.5313 mL | 1.3283 mL | |
| 60 mM | 0.0443 mL | 0.2214 mL | 0.4428 mL | 1.1069 mL | |
| 80 mM | 0.0332 mL | 0.1660 mL | 0.3321 mL | 0.8302 mL | |
| 100 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6641 mL |