Chemical Structure : RA306
货号: PC-72969Not For Human Use, Lab Use Only.
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.
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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.
分子量 | 571.737 | |
分子式 | C29H41N5O5S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Philippe Beauverger, et al. Cardiovasc Res. 2020 Feb 1;116(2):329-338.
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