NCG21 is a GPR120 agonist, which showed potent extracellularsignal-regulatedkinase (ERK) activation in a cloned GPR120 system. NCG21 potently activated ERK, intracellular calcium responses and GLP-1 secretion in murine enteroendocrine STC-1 cells that e
(2Z,3Z)-U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK ERKkinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellularsignal-regulatedkinase and mammalian target of rapamycin pathways.