CCG215022 |
Katalog-Nr.GC19090 |
CCG215022 ist ein Inhibitor der G-Protein-gekoppelten Rezeptorkinasen (GRKs) mit IC50-Werten von 0,15 ± 0,07 μM, 0,38 ± 0,06 μM und 3,9 ± 1 μM fÜr GRK2, GRK5 bzw. GRK1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1813527-81-9
Sample solution is provided at 25 µL, 10mM.
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.
CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2[1].
References:
[1]. Homan KT, et al. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally DesignedInhibitor. J Biol Chem. 2015 Aug 21;290(34):20649-59.
Average Rating: 5
(Based on Reviews and 21 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *