2410793-22-3
2410793-22-3 structure
- Name: GRK5-IN-3
- Chemical Name: GRK5-IN-3
- CAS Number: 2410793-22-3
- Molecular Formula: C23H21N7O3
- Molecular Weight: 443.46
- Catalog: Research Areas Others
- Create Date: 2022-09-18 19:47:29
- Modify Date: 2024-01-15 17:24:19
-
GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively[1].
| Name | GRK5-IN-3 |
|---|
| Description | GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.22 μM (GRK5), 0.41 μM (GRK6)[1] |
| In Vitro | GRK5 can be used to cancer, neurodegeneration, type 2 diabetes, heart failure and cardiovascular (CVD) research[1]. GRK5-IN-3 (Compound 5) (0-333 μM; 0-4 h) inhibits GRK5 in a time-dependent manner with IC50s of 59 μM (0 h), 11.3 μM (0.5 h), 6.2 μM (1 h), and 0.22 μM (4 h), respectively[1]. GRK5-IN-3 (0-333 μM; 0-4 h) also shows selectivity to human GRK5 over bovine GRK2 and bovine GRK1, with IC50s >100 μM (GRK1/2), respectively[1]. GRK5-IN-3 (0-333 μM; 0-4 h) exerts inhibition against GRK5, while light activated ROS as substrate, with IC50s of >100 μM (0 h), 4.2 μM (0.5 h), 3.4 μM (1 h), and 0.9 μM (4 h), respectively[1]. GRK5-IN-3 (0-333 μM; 4 h) shows no inhibitory effect on mutant GRK5 (GRK5-C474S, Cys474 mutated to serine), with IC50 values >100 μM[1]. |
| References |
| Molecular Formula | C23H21N7O3 |
|---|---|
| Molecular Weight | 443.46 |