GPER agonist G-1 (Tespria) is potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.
GPER agonist G-1 displays no activity at ERα and ERβ at concentrations up to 10 uM.
GPER agonist G-1 increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with IC50 of 0.7 and 1.6 nM respectively.
GPER agonist G-1 induces cell cycle arrest, DNA damage and cell death by the activation of the intrinsic apoptotic mechanism in H295R cells.
