| Bioactivity | GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research[1]. |
| Target | IC50: 1.1 ± 0.4 μM (GRK5), 1.8 ± 2 μM (GRK6), >100 μM (GRK2) |
| Invitro | GRK5-IN-4 (Compound 16d) (0-4 h) displays a marked increase in apparent potency as a function of time[1]. |
| Name | GRK5-IN-4 |
| CAS | 2410794-89-5 |
| Formula | C26H25N7O3 |
| Molar Mass | 483.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Rowlands RA, et al. Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. ACS Med Chem Lett. 2019 Nov 12;10(12):1628-1634. |
GRK5-IN-4
CAS: 2410794-89-5 F: C26H25N7O3 W: 483.52
GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) i
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