2767560-51-8
2767560-51-8 structure
- Name: A2AAR/HDAC-IN-1
- Chemical Name: A2AAR/HDAC-IN-1
- CAS Number: 2767560-51-8
- Molecular Formula: C24H21N7O2
- Molecular Weight: 439.47
- Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
- Create Date: 2022-10-09 16:23:02
- Modify Date: 2024-04-03 19:42:58
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A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].
| Name | A2AAR/HDAC-IN-1 |
|---|
| Description | A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1]. |
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| Related Catalog | |
| Target |
A2AR:163.5 ± 14 nM (Ki) A1AR:503.3 ± 14 nM (Ki) hA2B:>10000 nM (Ki) Adenosine A3 receptor:>10000 nM (Ki) HDAC1:145.3 ± 12 nM (IC50) HDAC2:240.2 ± 19 nM (IC50) HDAC3:443.5 ± 27 nM (IC50) HDAC6:>10000 nM (IC50) HDAC8:>10000 nM (IC50) |
| In Vitro | A2AAR/HDAC-IN-1 (compound 14c) (0-100 μM, 72 h) shows anti-proliferative activities against colon cancer cell lines, CT26 and MC38[1]. A2AAR/HDAC-IN-1 (0-5 μM, 24 h) increases histone acetylation[1]. A2AAR/HDAC-IN-1 shows moderate selectivity against A1AR (3-fold) and no significant binding for A2BAR and A3AR[1]. Cell Proliferation Assay[1] Cell Line: Colon cancer cell lines (CT26 and MC38) Concentration: 0-100 μM Incubation Time: 72 h Result: Displayed good cytotoxicity in CT26 and MC38 cells, with GI50 values of 0.29 ± 0.03 μM and 0.38 ± 0.03 μM, respectively. Western Blot Analysis[1] Cell Line: MC38 mouse colon cancer cells Concentration: 0, 0.1, 1, and 5 μM Incubation Time: 24 h Result: Increased histone H3 and H4 acetylation in a concentration-dependent manner. |
| References |
| Molecular Formula | C24H21N7O2 |
|---|---|
| Molecular Weight | 439.47 |