2767560-94-9
2767560-94-9 structure
- Name: A2AAR/HDAC-IN-2
- Chemical Name: A2AAR/HDAC-IN-2
- CAS Number: 2767560-94-9
- Molecular Formula: C23H26N6O4
- Molecular Weight: 450.49
- Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
- Create Date: 2022-10-10 19:54:47
- Modify Date: 2024-04-12 14:09:02
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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[1].
| Name | A2AAR/HDAC-IN-2 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
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) |
| 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]. Cell Proliferation Assay[1] Cell Line: MC38 and CT26 cells Concentration: 5 nM-100 µM Incubation Time: 72 h 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. Western Blot Analysis[1] Cell Line: MC38 cells Concentration: 0.1, 1, 5, 10 µM Incubation Time: 24 h Result: Significantly increases histone H3 and H4 acetylation at 10 µM and in a concentration-dependent manner. |
| References |
| Molecular Formula | C23H26N6O4 |
|---|---|
| Molecular Weight | 450.49 |