DC70727 |
RA306
|
RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes. |