Potent and selective GPER agonist (Ki
= 11 nM, EC50
= 2 nM); displays no activity at ERα
at concentrations up to 10 μ
M. Increases cytosolic Ca2+
and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50
values are 0.7 and 1.6 nM respectively) in vitro
. Blocks MCF-1 cell cycle progression at the G1
phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis.
Blasko et al.
The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.
Ariazi et al.
Cancer Res., 2010;70:1184
G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells.
Albanito et al.
Cancer Res., 2007;67:1859
Virtual and biomolecular screening converge on a selective agonist for GPR30.
Bologa et al.
Nature Chem.Biol., 2006;2:207
The citations listed below are publications that use Tocris products. Selected citations for G-1 include:
Showing Results 1 - 10 of 11