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CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50 values of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively. 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.
| Molecular Weight | 499.5 |
| Formula | C26H22FN7O3 |
| CAS Number | 1813527-81-9 |
| Solubility (25°C) | DMSO: ≥ 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PKA Products |
|---|
| H-89 Dihydrochloride
H-89 dihydrochloride is a selective inhibitor of protein kinase A (PKA) with an IC50 value of 135 nM. |
| Bucladesine Sodium Salt
Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. |
| H-89
H-89 is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
| 8-Bromo-cAMP sodium salt
8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator. |
| 5-Iodotubercidin
5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. |
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