G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a K_i of 20 nM^[1][2]. IC50 & Target: Ki: 20 nM (GPER/GPR30)^[2] In Vitro: G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines^[1].
G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines^[1]. In Vivo: G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice^[1].