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 No.: 2652579-44-5
- Formule: C19H16N6OS
- Masse moléculaire:376.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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HDAC2 14 nM (IC50) |
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.
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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Masse moléculaire 376.43
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC2-IN-3 Related Classifications
HY-182321 Related Classifications
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