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.
For research use only. We do not sell to patients.
- CAS No.: 2767560-94-9
- Formula: C23H26N6O4
- Molecular Weight:450.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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] |
In Vitro
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.
Chemical Information
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CAS No. 2767560-94-9
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Molecular Weight 450.49
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A2AAR/HDAC-IN-2 Related Classifications
HY-143325 Related Classifications
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