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. Nr.: 2767560-94-9
- Formel: C23H26N6O4
- Molecular Weight:450.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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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) |
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
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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.
Chemical Information
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CAS. Nr. 2767560-94-9
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Molecular Weight 450.49
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
A2AAR/HDAC-IN-2 Related Classifications
HY-143325 Related Classifications
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