G15, GPER Antagonist

G-15 is a cell permeable, nonsteroidal, high-affinity, selective antagonist of GPER that binds GPER with affinity of about 20-30 nM, 1/3 that of G-1 (AZ00001-G15)). G15 inhibits GPER-mediated calcium mobilization in human breast carcinoma SKBr3 cells (IC50 ~190 nM against stimulation by either 100 nM G-1 or 30 nM 17β-estradiol) in vitro and blocks G-1-induced (0.5 nmol per animal via s.c.) uterine epithelial proliferation (by ≥76% with ≥7.4 nmol G15 per animal via s.c.) in ovariectomized mice in vivo.