Table 1.
IC50/ EC50 (in μM) derived using data acquired in various bovine cardiac systems from ATPase and Single ATP turnover experiments | |||
---|---|---|---|
Para-nitroblebbistatin | Mavacamten | ||
0μM blebbistatin |
10μM blebbistatin |
||
Basal ATPase (BcSTF) | 2.37±0.12* | 0.63±0.05 | |
Actin-activated ATPase (BcSTF) | 4.81±0.16* | 1.25±0.11 | |
Myofibrillar ATPase (BcMF) | 4.05±0.34* | 0.50±0.05 | |
SRX Amplitude, Aslow (BcSTF) | >12.5* | 1.21±0.35 | 0.63±0.07* |
DRX ATPase Rate, kfast (BcSTF) | >12.5* | 0.43±0.03 | 0.64±0.12 |
SRX ATPase Rate, kslow (BcSTF) | >12.5 | >12.5 | >12.5 |
SRX Amplitude, Aslow (BcMF) | >12.5* | 4.30±0.31 | |
DRX ATPase Rate, kfast (BcMF) | >12.5* | 0.59±0.08 | |
SRX ATPase Rate, kslow (BcMF) | >12.5 | >12.5 |
Nomenclature is as follows: BcSTF refers to bovine β-cardiac synthetic thick filaments; BcMF, bovine cardiac myofibrils. Data are expressed as mean±SEM (n≥8 from two experiments that used single preparation of the same purification). The IC50/EC50 values of both blebbistatin and para-nitroblebbistain are statistically different from mavacamten based on a student’s t-test (*p<0.001). The Hill coefficient measured in these experiments is always between 2–4.