serca2a

SERCA2a activator 1 is a sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a activator. SERCA2a activator 1 decreases phospholamban inhibition and enhances the systolic and diastolic functions of the heart.

SERCA2a activator 2 (Compound 25) is a potent activator of SERCA2a (cardiac type) and also activates SERCA1a (skeletal muscle type). Under [Ca²⁺]MAX conditions, it enhances SERCA2a ATPase activity and facilitates Ca²⁺ uptake with EC₅₀ values of 4 μM and 0.80 μM, respectively. It consistently activates under near-physiological [Ca²⁺]MID conditions as well. Furthermore, SERCA2a activator 2 exhibits low cytotoxicity, making it useful for researching diseases such as heart failure.

RyR2 stabilizer-1 (Compound12a) is a potent stabilizer of RyR2 and an activator of SERCA2a, with EC50 values of 2.7 μM for RyR2 and 383 nM for SERCA2. This compound inhibits the leakage of Ca2+ through SR RyR2 while promoting the reuptake of Ca2+ into the SR by SERCA2, suggesting its potential in preventing arrhythmias.

Multi-target kinase-IN-6 is a multi-target kinase inhibitor. It can inhibit cardiac RyR2 and NaV1.5 channels while stimulating the activity of the SERCA2a pump. Multi-target kinase-IN-6 is applicable in research on cardiovascular diseases, including heart failure.

N106 is an activator of the SUMO-activating enzyme, E1 ligase, and triggers intrinsic sumoylation of SERCA2a. N106 can be used in studies about heart failure.