G-15

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER) antagonist with a Ki of 20 nM[1][2].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

Ki: 20 nM (G-protein-coupled estrogen receptor)[2]

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]. Cell Proliferation Assay[1] Cell Line: A549, H1793 cell lines Concentration: 0.1, 1, 10 μM (combination with 10 nM E2) Incubation Time: 2 days Result: Inhibited GPER-mediated proliferation stimulated by E2. Western Blot Analysis[1] Cell Line: A549, H1793 cell lines Concentration: 1 μM (combination with 10 nM E2 and 10 nM G1) Incubation Time: 48 hours Result: Inhibited the response of GPER stimulated by E2 and G1.

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]. Animal Model: Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1] Dosage: 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) Administration: Subcutaneous injection; twice a week for 14 weeks Result: The number of tumor nodules decreased in the E2+Ful+G15 group.

[1]. Liu C, et al. G-Protein-Coupled Estrogen Receptor Antagonist G15 Decreases Estrogen-Induced Development of Non-Small Cell Lung Cancer. Oncol Res. 2019 Feb 21;27(3):283-292

[2]. Girgert R, et al. Estrogen Signaling in ERα-Negative Breast Cancer: ERβ and GPER. Front Endocrinol (Lausanne). 2019 Jan 9;9:781.