CCG258208
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research[1].
Product Specifications
CAS Number
[2055990-90-2]
Product Name Alternative
GRKs-IN-1
UNSPSC
12352005
Target
G Protein-coupled Receptor Kinase (GRK)
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Neuroscience-Neuromodulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/grk2-in-1.html
Solubility
10 mM in DMSO
Smiles
FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1
Molecular Formula
C24H25FN4O4
Molecular Weight
452.48
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
GRK2
Curated Selection
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