G-1

Cat. No. 3577

G-1 C21H18BrNO3 [881639-98-1]

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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 Activity

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.

Technical Data

M.Wt:
412.28
Formula:
C21H18BrNO3
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
881639-98-1

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Ariazi et al (2010) The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res. 70 1184. PMID: 20086172.

Blasko et al (2009) Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. J.Neuroimmunol. 214 67. PMID: 19664827.

Albanito et al (2007) 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. Cancer Res. 67 1859. PMID: 17308128.

Bologa et al (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol. 2 207.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for G-1 include:

Chimento et al (2015) GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Cell Death Dis 6 19190. PMID: 26131713.

Lappano et al (2015) A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models. Cell Death Dis 8 1237. PMID: 26183213.

Santolla et al (2015) SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer. Sci Rep 6 e1834. PMID: 26225773.

Villa et al (2015) Estrogen accelerates the resolution of inflammation in macrophagic cells. Breast Cancer Res 5 15224. PMID: 26477569.

Yuan et al (2015) Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamoxifen resistance through cancer-associated fibroblast-derived fibronectin and β1-integrin signaling pathway in tumor cells. Dis Model Mech 17 69. PMID: 25990368.

An et al (2014) Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. Brain Behav 15 10479. PMID: 24921706.

Anchan et al (2014) GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice. Am J Physiol Renal Physiol 4 51. PMID: 24653954.

Nag and Mokha (2014) 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. Oncotarget 267 122. PMID: 24613724.

Chimento et al (2013) Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells. Int J Mol Sci 4 e747. PMID: 23907461.

Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376. PMID: 24327954.

Duncan et al (2012) 2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A 109 21034. PMID: 23213242.

Do you know of a great paper that uses G-1 from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: G-1, supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER, Tocris Bioscience, Estrogen (GPER) Receptor Agonist products

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