Cat. No. 5642
Chemical Name: 3-[[[4-Methyl-5-(4-pyridinyl)-4H-1,
Biological ActivityPotent and selective GRK2/3 inhibitor (IC50 values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Lowe et al (2015) Role of G protein-coupled receptor kinases 2 and 3 in μ-opioid receptor desensitization and internalization. Mol.Pharmacol. 88 347. PMID: 26013542.
Thal et al (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol.Pharmacol. 80 294. PMID: 21596927.
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Keywords: CMPD101, supplier, potent, selective, GRK2, GRK3, inhibitors, inhibits, receptors, GPCRs, desensitization, kinases, Tocris Bioscience, G Protein (Heterotrimeric) Inhibitor products