A2AAR/HDAC-IN-2
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.
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- CAS 番号: 2767560-94-9
- 分子式: C23H26N6O4
- 分子量:450.49
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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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Help & FAQs
Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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HDAC1 18.5 nM (IC50) |
HDAC2 16.0 nM (IC50) |
HDAC3 13.6 nM (IC50) |
HDAC6 2.1 nM (IC50) |
HDAC8 1408.9 nM (IC50) |
A1AR 105.6 nM (Ki) |
A2AAR 10.3 nM (Ki) |
A2BAR 513.0 nM (Ki) |
A3AR ＞10 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | GI50 |
12.61 μM
Compound: 30c
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Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
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[PMID: 35390714] |
| MC-38 | GI50 |
12.16 μM
Compound: 30c
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Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
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[PMID: 35390714] |
体外実験
A2AAR/HDAC-IN-2 (compound 30c) (5 nM-100 µM; 72 h) shows anti-proliferative activity, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively[1].
A2AAR/HDAC-IN-2 (0.1, 1, 5, 10 µM; 24 h) increases histone H3 and H4 acetylation in a concentration-dependent manner in MC38 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MC38 and CT26 cells
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Concentration:5 nM-100 µM
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Incubation Time:72 h
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Result:Showed good anti-proliferative activity in cancer cell lines, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively.
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Cell Line:MC38 cells
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Concentration:0.1, 1, 5, 10 µM
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Incubation Time:24 h
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Result:Significantly increases histone H3 and H4 acetylation at 10 µM and in a concentration-dependent manner.
化学情報
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CAS 番号 2767560-94-9
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分子量 450.49
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分子式 C23H26N6O4
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SMILES
NC1=NC(C2=CC=CO2)=C3C=NN(C3=N1)CC4=CC=CC(OCCCCCCC(NO)=O)=C4
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
A2AAR/HDAC-IN-2 関連分類
HY-143325 関連分類
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