Calmodulin Activator

Setmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide monoacetate activates the CaMKK2/AMPK signaling pathway. Setmelanotide monoacetate mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide monoacetate is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.

DC-120 is an ATP-competitive AKT inhibitor, with particular activity against AKT1 (an IC₅₀ of 0.153 μM). DC-120 functionally blocks AKT kinase activity and reduces the phosphorylation levels of FOXO3a and GSK-3β. DC-120 induces cancer cell apoptosis (apoptosis) and inhibits cancer cell proliferation. DC-120 activates the mTORC1 pathway via the Ca²⁺/calmodulin (calmodulin)/hVps34 signaling pathway. DC-120 abrogates AKT-mediated inhibition of CRAF, thereby activating the MEK/ERK MAPK pathway. DC-120 exerts anti-tumor activity in a nude mouse hepatocellular carcinoma xenograft model. DC-120 can be used for hepatocellular carcinoma-related research.