AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM.
AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93).
In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i.
AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.
Cat.No
DC70209
Name
AS105
Chemical Properties
CAS
1026029-18-4
Formula
C18H18CLN5
MW
339.822021961212
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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