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RA306

Chemical Structure : RA306

CAS No.:

RA306 (RA-306, RA 306)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 571.737
    Formula C29H41N5O5S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (R)-2-(2-((4-(4-(2-(hydroxymethyl)morpholino)piperidin-1-yl)-2-methoxyphenyl)amino)-7-isopropoxythieno[3,2-d]pyrimidin-6-yl)propan-2-ol

    References

    1. Philippe Beauverger, et al. Cardiovasc Res. 2020 Feb 1;116(2):329-338.

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