CCG258208 hydrochloride (Synonyms: GRK2-IN-1 hydrochloride) |
| Catalog No.GC62891 |
Le chlorhydrate de CCG258208 (GRK2-IN-1) est un inhibiteur puissant et sélectif de GRK2 (récepteur couplé aux protéines G kinase 2) (IC50 = 30 nM) tout en maintenant une sélectivité de 230 fois par rapport À GRK5 (IC50 = 7,09 μM) et plus de 2500- plier la sélectivité sur GRK1 (IC50 = 87,3 μM), PKA et ROCK1.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1].
[1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.
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