Chemical Name: (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone
Biological ActivityG-1 is a potent and selective GPER agonist (Ki = 11 nM, EC50 = 2 nM); displays no activity at ERα and ERβ at concentrations up to 10 μM. 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. Also inhibits glutamate-induced autophagy and neuronal loss in cultured primary cortical neurons.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-OE and selective GPR30 ligand G-1 in ovarian cancer cells.
Albanito et al.
Cancer Res., 2007;67:1859
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
Virtual and biomolecular screening converge on a selective agonist for GPR30.
Bologa et al.
Nature Chem.Biol., 2006;2:207
Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate.
Yue et al.
ACS Chem.Neurosci, 2019;10:4227
Citations for G-1
The citations listed below are publications that use Tocris products. Selected citations for G-1 include:
19 Citations: Showing 1 - 10
TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor.
Authors: Cortes Et al.
Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1.
Authors: Loiola Et al.
Front Endocrinol (Lausanne) 2019;10:420
Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin.
Authors: Meseke Et al.
Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol.
Authors: Caballero Et al.
Sci Rep 2017;7:40981
GPR30 decreases with vascular aging and promotes vascular smooth muscle cells maintaining differentiated phenotype and suppressing migration via activation of ERK1/2.
Authors: Huang Et al.
Onco Targets Ther 2016;9:3415
A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models.
Authors: Lappano Et al.
Cell Death Dis 2015;8:1237
SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer.
Authors: Santolla Et al.
Sci Rep 2015;6:e1834
GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo.
Authors: Chimento Et al.
Cell Death Dis 2015;6:19190
Estrogen accelerates the resolution of inflammation in macrophagic cells.
Authors: Villa Et al.
Breast Cancer Res 2015;5:15224
Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat.
Authors: Mazzuca Et al.
J Pharmacol Exp Ther 2015;352:291
Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamox. resistance through cancer-associated fibroblast-derived fibronectin and
Authors: Yuan Et al.
Dis Model Mech 2015;17:69
GPER mediates activation of HIF1α/VEGF signaling by estrogens.
Authors: Francesco Et al.
Cancer Res 2014;74:4053
GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice.
Authors: Anchan Et al.
Am J Physiol Renal Physiol 2014;4:51
Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility.
Authors: Sandner Et al.
Activation of a Gq-coupled membrane estrogen receptor rapidly attenuates α2-adrenoceptor-induced antinociception via an ERK I/II-dependent, non-genomic mechanism in the female rat.
Authors: Nag and Mokha
Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor.
Authors: An Et al.
Brain Behav 2014;15:10479
Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells.
Authors: Chimento Et al.
Int J Mol Sci 2013;4:e747
Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
Authors: Engelstoft Et al.
Mol Metab 2013;2:376
2-MethoxyOE inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation.
Authors: Duncan Et al.
Proc Natl Acad Sci U S A 2012;109:21034
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