GRK1: Small Molecules and Peptides
G protein-coupled receptor kinases (GRKs) are important modulators of G protein-coupled receptor (GPCR) signaling. Receptor phosphorylation by specific GRKs plays a key role in triggering rapid desensitization. The GRK family consists of 7 isoforms that share a central catalytic domain with homology to other serine/threonine kinases. The catalytic domain is flanked by an amino-terminal RGS domain of 183 - 188 amino acids and a carboxyl-terminus of variable length. GRK1 and GRK7 are members of the rhodopsin kinase or visual GRK subfamily.
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GRK1: Small Molecules and Peptides
G protein-coupled receptor kinases (GRKs) are important modulators of G protein-coupled receptor (GPCR) signaling. Receptor phosphorylation by specific GRKs plays a key role in triggering rapid desensitization. The GRK family consists of 7 isoforms that share a central catalytic domain with homology to other serine/threonine kinases. The catalytic domain is flanked by an amino-terminal RGS domain of 183 - 188 amino acids and a carboxyl-terminus of variable length. GRK1 and GRK7 are members of the rhodopsin kinase or visual GRK subfamily.
Potent and selective GRK2/3 inhibitor
| Chemical Name: | 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide |
| Purity: | ≥98% (HPLC) |