HDAC-IN-100
HDAC-IN-100 is a histone deacetylase inhibitor with an IC50 of 0.038 μM against HDAC1, 0.283 μM against HDAC2, and 0.586 μM against HDAC3. HDAC-IN-100 acts as a chemosensitizer and apoptosis inducer, activates caspase 3/7, and reverses Cisplatin (HY-17394) resistance. HDAC-IN-100 exerts antiproliferative effects in ovarian cancer cells and squamous cancer cells. HDAC-IN-100 is applicable for research related to ovarian cancer, squamous cell carcinoma, and Cisplatin (HY-17394)-resistant squamous cell carcinoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 2390474-88-9
- 分子式: C32H33N5O3
- 分子量:535.64
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
IC50 & Target
[1]|
HDAC1 0.038 μM (IC50) |
HDAC2 0.283 μM (IC50) |
HDAC3 0.586 μM (IC50) |
Caspase-3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.48 μM
Compound: 2a
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Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
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[PMID: 31762274] |
体外実験
HDAC-IN-100 (compound 2a) (72 h) reduces the viability of human cancer cells A2780 (IC50 2.40 μM) and Cal27 (IC50 1.60 μM)[1].
HDAC-IN-100 (0-100 μM; 18 h) potently inhibits cellular HDAC activity in human cancer cells A2780 (IC50 0.48 μM) and Cal27 (IC50 0.11 μM)[1].
HDAC-IN-100 (0.5 μM; 48 h) exerts a strong synergistic effect with Cisplatin (HY-17394) to reduce the viability of Cal27 cells and Cisplatin-resistant Cal27CisR cells, and completely reverses the Cisplatin resistance of Cal27CisR cells[1].
HDAC-IN-100 (0.5 μM; 48 h) significantly increases the apoptosis levels in Cal27 cells and cisplatin (HY-17394)-resistant Cal27CisR cells[1].
HDAC-IN-100 (0.5 μM; 24 h) induces hyperacetylation of histone H3 in Cal27 cells and cisplatin (HY-17394)-resistant Cal27CisR 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 tongue squamous cell carcinoma Cal27 cells, cisplatin-resistant Cal27CisR cells
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Concentration:0.5 μM
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Incubation Time:48 h (pretreatment); 72 h (Cisplatin incubation)
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Result:Reduced the cisplatin IC50 from 9.79 μM to 1.26 μM in Cal27 cells.
Reduced the cisplatin IC50 from 63.2 μM to 8.42 μM in Cal27CisR cells,.
Showed synergistic interaction with Cisplatin, with strong synergism observed at multiple concentration combinations.
化学情報
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CAS 番号 2390474-88-9
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分子量 535.64
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分子式 C32H33N5O3
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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.
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)
HDAC-IN-100 関連分類
HY-P11678 関連分類
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