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.
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- CAS. Nr.: 2652579-44-5
- Formel: C19H16N6OS
- Molecular Weight:376.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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. Nr. 2652579-44-5
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Molecular Weight 376.43
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Formel C19H16N6OS
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)