HDAC2-IN-4
HDAC2-IN-4 is a HDAC2 inhibitor with an IC50 of 4.2 nM against human HDAC2. HDAC2-IN-4 binds to the active site of HDAC2 via hydrogen bonding and hydrophobic interactions, forming a thermodynamically stable and kinetically compatible protein-ligand complex to inhibit enzymatic activity. HDAC2-IN-4 inhibits cancer cell proliferation and exhibits low toxicity to normal cells. HDAC2-IN-4 can be used in studies related to human endocervical adenocarcinoma and Burkitt lymphoma.
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- Fòrmula: C19H28N2O5
- Peso molecular:364.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
hHDAC2 4.2 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
5.07 μM
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Antiproliferative activity against human endocervical adenocarcinoma HeLa cells assessed by resazurin assay after 72 h incubation with the compound followed by 3 h resazurin incubation.
Antiproliferative activity against human endocervical adenocarcinoma HeLa cells assessed by resazurin assay after 72 h incubation with the compound followed by 3 h resazurin incubation.
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42520173 |
| Raji | IC50 |
1.87 μM
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Antiproliferative activity against human Burkitt's lymphoma Raji cells assessed by resazurin assay after 72 h incubation with the compound followed by 3 h resazurin incubation.
Antiproliferative activity against human Burkitt's lymphoma Raji cells assessed by resazurin assay after 72 h incubation with the compound followed by 3 h resazurin incubation.
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42520173 |
In Vitro
HDAC2-IN-4 (compound 23e) (0.1-100 μM; 1 h) potently inhibits purified human HDAC2 protein, with an IC50 of 4.2 nM[1].
HDAC2-IN-4 (500 ns) forms a thermodynamically stable and kinetically compatible complex with human HDAC2 protein[1].
HDAC2-IN-4 (0.1-250 μM; 72 h) potently inhibits the proliferation of HeLa and Raji cancer cells, with IC50 values of 5.07 μM and 1.87 μM, respectively, while exhibiting low toxicity toward non-cancerous Hek293T and DF cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human endocervical adenocarcinoma (HeLa) cells, human Burkitt's lymphoma (Raji) cells, human embryonic kidney (Hek293T) non-cancer cells, primary human dermal fibroblasts (DF) non-cancer cells
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Concentration:0.1, 1, 10, 50 and 250 μM
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Incubation Time:72 h
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Result:Exhibited pronounced antiproliferative activity against HeLa cells with an IC50 of 5.07 μM.
Exhibited pronounced antiproliferative activity against Raji cells with an IC50 of 1.87 μM.
Showed low toxicity against non-cancer Hek293T and DF cells, demonstrating selective cytotoxicity toward malignant cells.
Chemical Information
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Peso molecular 364.44
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Fòrmula C19H28N2O5
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SMILES
O=C(OCCCC)C1=CC=C(NC(CCCCCCC(NO)=O)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC2-IN-4 Related Classifications
HY-187813 Related Classifications
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