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G-1

Catalog #: 3577
33 Citations Datasheet / COA / SDS
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G-1 | CAS No. 881639-98-1 | Estrogen and Related Receptor Agonists
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Description: Potent and selective GPER agonist

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

Purity: ≥98%

Product Details
Citations (33)
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Biological Activity

G-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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. GPER signalling in both cancer-associated fibroblasts and breast cancer cells mediates a feedforward IL1?/IL1R1 response
    P De Marco, R Lappano, EM Francesco, F Cirillo, M Pupo, S Avino, A Vivacqua, S Abonante, D Picard, M Maggiolini
    Sci Rep, 2016;6(0):24354.
  2. Pregnancy Augments G Protein Estrogen Receptor (GPER) Induced Vasodilation in Rat Uterine Arteries via the Nitric Oxide - cGMP Signaling Pathway.
    Tropea T, De Francesco E, Rigiracciolo D, Maggiolini M, Wareing M, Osol G, Mandala M
    PLoS ONE, 2015;10(11):e0141997.
  3. 17 beta-Estradiol activates GPER- and ESR1-dependent pathways inducing apoptosis in GC-2 cells, a mouse spermatocyte-derived cell line.
    Chimento A, Sirianni R, Casaburi I, Ruggiero C, Maggiolini M, Ando S, Pezzi V
    Mol. Cell. Endocrinol., 2012;355(1):49-59.
  4. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes.
    Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M
    J Biol Chem, 2012;287(32):26817-28.
  5. 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
  6. Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis.
    Blasko et al.
    J.Neuroimmunol., 2009;214:67
  7. The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.
    Ariazi et al.
    Cancer Res., 2010;70:1184
  8. Virtual and biomolecular screening converge on a selective agonist for GPR30.
    Bologa et al.
    Nature Chem.Biol., 2006;2:207
  9. 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

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Citations for G-1

The citations listed below are publications that use Tocris products. Selected citations for G-1 include:

33 Citations: Showing 1 - 10

  1. Anti-Inflammatory Actions of G-Protein-Coupled Estrogen Receptor 1 (GPER) and Brain-Derived Estrogen Following Cerebral Ischemia in Ovariectomized Rats.
    Authors: Jing Et al.
    Biology (Basel)  2023;12
  2. ERα-independent NRF2-mediated immunoregulatory activity of tamoxifen.
    Authors: Massimo Et al.
    Biomed Pharmacother  2021;144:112274
  3. GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERα-positive breast cancer cells.
    Authors: Lin Et al.
    Aging (Albany NY)  2021;13:16178-16197
  4. Sex Differences in the Pro-Angiogenic Response of Human Endothelial Cells: Focus on PFKFB3 and FAK Activation.
    Authors: Andrea Et al.
    Front Pharmacol  2021;11:587221
  5. Utilizing Designed Receptors Exclusively Activated by Designer Drug Chemogenetic Tools to Identify Beneficial G Protein-Coupled Receptor Signaling for Fibrosis.
    Authors: Tzu-Ming Et al.
    J Pharmacol Exp Ther  2020;375:357-366
  6. G Protein-Coupled Estrogen Receptor Mediates Cell Proliferation through the cAMP/PKA/CREB Pathway in Murine Bone Marrow Mesenchymal Stem Cells.
    Authors: Mei-Ling Et al.
    Int J Mol Sci  2020;21
  7. G-protein-coupled estrogen receptor activation upregulates interleukin-1 receptor antagonist in the hippocampus after global cerebral ischemia: implications for neuronal self-defense.
    Authors: Bin Et al.
    J Neuroinflammation  2020;17:45
  8. GPER Activation Inhibits Cancer Cell Mechanotransduction and Basement Membrane Invasion via RhoA.
    Authors: David A Et al.
    Cancers (Basel)  2020;12
  9. Essential and sex-specific effects of mGluR5 in ventromedial hypothalamus regulating estrogen signaling and glucose balance.
    Authors: Jamie Et al.
    Proc Natl Acad Sci U S A  2020;117:19566-19577
  10. Low-dose Bisphenol-A regulates inflammatory cytokines through GPR30 in mammary adipose cells.
    Authors: Francesco Et al.
    J Mol Endocrinol  2019;63:273-283
  11. TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor.
    Authors: Cortes Et al.
    Oncogene  2019;38:2910
  12. G protein-coupled estrogen receptor activates cell type-specific signaling pathways in cortical cultures: relevance to the selective loss of astrocytes.
    Authors: Cláudio Et al.
    J Neurochem  2019;149:27-40
  13. 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
  14. Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin.
    Authors: Meseke Et al.
    Eneuro  2018;5
  15. 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
  16. 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
  17. Estrogen and G protein-coupled estrogen receptor agonist G-1 cause relaxation of human gallbladder.
    Authors: Yi-Chen Et al.
    Ci Ji Yi Xue Za Zhi  2016;28:54-58
  18. 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
  19. SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer.
    Authors: Santolla Et al.
    Sci Rep  2015;6:e1834
  20. 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
  21. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res  2015;5:15224
  22. 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
  23. 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
  24. GPER mediates activation of HIF1α/VEGF signaling by estrogens.
    Authors: Francesco Et al.
    Cancer Res  2014;74:4053
  25. 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
  26. Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility.
    Authors: Sandner Et al.
    Andrology  2014;2:695
  27. 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
    Oncotarget  2014;267:122
  28. Activation of membrane estrogen receptors attenuates opioid receptor-like1 receptor-mediated antinociception via an ERK-dependent non-genomic mechanism.
    Authors: S Et al.
    Neuroscience  2014;255:177-90
  29. 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
  30. Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells.
    Authors: Chimento Et al.
    Int J Mol Sci  2013;4:e747
  31. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
    Authors: Engelstoft Et al.
    Mol Metab  2013;2:376
  32. GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer.
    Authors: Manran Et al.
    Breast Cancer Res  2013;15:R114
  33. 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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