| Bioactivity | CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle[1]. | ||||||||||||
| Target | IC50: 3.8 nM (human GRK5), 19 nM (GRK5-C474S), 4.8 μM (bovine GRK2) | ||||||||||||
| Invitro | Human GRKs (GRK1−GRK7) are classified into three subfamilies: GRK1 (GRK1 and GRK7), GRK2 (GRK2 and GRK3), and GRK4 (GRK4, GRK5, and GRK6)[1].CCG273441 (compound 9j) shows moderate potency (GRK5 IC50=3.8 nM) but 1000-fold selectivity over GRK2 (IC50=4.8 μM)[1]. | ||||||||||||
| Name | CCG273441 | ||||||||||||
| CAS | 2750414-35-6 | ||||||||||||
| Formula | C26H24ClFN4O3 | ||||||||||||
| Molar Mass | 494.95 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Rowlands RA, et al. Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. J Med Chem. 2021 Jan 14;64(1):566-585. |
CCG273441
CAS: 2750414-35-6 F: C26H24ClFN4O3 W: 494.95
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG
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