G36

Description: G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17beta-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERalpha or ERbeta. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERalpha and ERbeta in complex biological systems. Target: Estrogen Receptor/ERR. Smiles: [H][C@]12CC=C[C@@]1([H])c1cc(ccc1N[C@H]2c1cc2OCOc2cc1Br)C(C)C. References: Filardo, E.J., and Thomas, P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 153(7), 2953-2962 (2012).