N106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research.In Vitro: N106 treatment increases contractile properties of cultured rat cardiomyocytes. N106 increases cell contractility, calcium-transient SERCA2a’s ATPase activity and SUMOylation within 10?min of exposure, and these effects are sustained at 24?h in cardiomyocytes.In Vivo: In a murine model, the half-life of N106 is determined to be ～65.4?min with a Cmax of ～2.24?μM when the mice received 10?mg/kg of N106 by intravenous injection. The oral bioavailability (F%) is 56% and 50%, and terminal elimination half-life (t1/2) is 19?min. In vivo, N106 (10 mg/kg) increases cardiac SERCA2A SUMOylation, and significantly improves ventricular function in mice with heart failure.