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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2652579-44-5
- 分子式: C19H16N6OS
- 分子量:376.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
HDAC2 14 nM (IC50) |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 2652579-44-5
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分子量 376.43
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)