Cat. No.: HY-103449

G15

42 Cited Publications

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Based on 42 publication(s) in Google Scholar

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a K_i of 20 nM.

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Pureté: 99.0%
CAS No.: 1161002-05-6
Formule: C₁₉H₁₆BrNO₂
Masse moléculaire:370.24

Stockage:

-20°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

G15 Chemical Structure

CAS No.: 1161002-05-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (42)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a K_i of 20 nM^[1]^[2].

IC₅₀ & Target

Ki: 20 nM (GPER/GPR30)^[2]

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-BR-3	IC₅₀	185 nM Compound: G15	Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of G1-mediated calcium mobilization Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of G1-mediated calcium mobilization	[PMID: 19430488]
SK-BR-3	IC₅₀	190 nM Compound: G15	Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of E2-mediated calcium mobilization Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of E2-mediated calcium mobilization	[PMID: 19430488]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1161002-05-6
Appearance Solid
Masse moléculaire 370.24
Formule C₁₉H₁₆BrNO₂
Color White to off-white
SMILES

BrC1=C([C@@H]2NC3=C(C=CC=C3)[C@@]4([H])[C@]2([H])CC=C4)C=C5OCOC5=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Publications (42)

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Cell Death Dis

Dehydroepiandrosterone exacerbates nigericin-induced abnormal autophagy and pyroptosis via GPER activation in LPS-primed macrophages. [Abstract]

2022 Apr 19;13(4):372. PMID: 35440074

G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372. [Abstract]

J774A.1 cells were pre-treated with DHEA (50 μM) in the presence or absence of the GPER inhibitor G15 (1 μM) for 1 h, then stimulated with LPS for 4 h. The TLR4, p-ERK/ERK, LC3, p62, p-mTOR, and p-AMPK protein expression levels were measured by western blotting and quantified by Image J software.

G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372. [Abstract]

J774A.1 cells were pre-treated with G1 (1 μM) for 1 h, then stimulated with LPS for 4 h, and the indicated protein expression levels were measured by western blotting and quantified by Image J software.

G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372. [Abstract]

J774A.1 cells were pre-treated with DHEA (50 μM) in the presence or absence of the GPER inhibitor G15 (1 μM) for 1 h, then stimulated with LPS for 4 h, PI-positive dead cells in 5 randomly selected fluorescence microscope images were counted by Image J software, scale bar = 200 μm.
J Hazard Mater

Selenium restored mitophagic flux to alleviate cadmium-induced hepatotoxicity by inhibiting excessive GPER1-mediated mitophagy activation. [Abstract]

2024 Aug 15:475:134855. PMID: 38880044
Environ Int

Neonicotinoid insecticides promote breast cancer progression via G protein-coupled estrogen receptor: In vivo, in vitro and in silico studies. [Abstract]

2022 Dec:170:107568. PMID: 36240625
Environ Pollut

G protein-coupled estrogen receptor activation by bisphenol-A disrupts lipid metabolism and induces ferroptosis in the liver. [Abstract]

2023 Oct 1:334:122211. PMID: 37454720
Environ Pollut

BPA modulates the WDR5/TET2 complex to regulate ERβ expression in eutopic endometrium and drives the development of endometriosis. [Abstract]

2021 Jan 1;268(Pt B):115748. PMID: 33022573
Biochem Pharmacol

Gut microbiota-derived isoxanthohumol metabolite, 8-prenylnaringenin, mitigates endothelial dysfunction in Angiotensin II-induced hypertension through G protein-coupled estrogen receptor-mediated eNOS activation. [Abstract]

2026 Apr:246:117728. PMID: 41571201
Biochem Pharmacol

Effects of G protein-coupled estrogen receptor on hydrogen sulfide production and cystathionine γ-lyase expression in human endothelial cells. [Abstract]

2025 Sep 19;242(Pt 3):117354. PMID: 40976431
Biochem Pharmacol

G protein-coupled estrogen receptor regulates the KLF2-dependent eNOS expression by activating of Ca2+ and EGFR signaling pathway in human endothelial cells. [Abstract]

2021 Oct:192:114721. PMID: 34363795
Life Sci

Genistein accelerates glucose catabolism via activation the GPER-mediated cAMP/PKA-AMPK signaling pathway in broiler chickens. [Abstract]

2022 Aug 15:303:120676. PMID: 35640778
Pharm Biol

Tongmai Yangxin pill alleviates myocardial no-reflow by activating GPER to regulate HIF-1α signaling and downstream potassium channels. [Abstract]

2023 Dec;61(1):499-513. PMID: 36896463

G15 purchased from MedChemExpress. Usage Cited in: Pharm Biol. 2023 Dec;61(1):499-513. [Abstract]

TMYX enhanced the dilation function of coronary microvessels in vitro, but this effect was inhibited by G-15.
Eur J Pharmacol

Estradiol reduced 5-HT reuptake by downregulating the gene expression of Plasma Membrane Monoamine Transporter (PMAT, Slc29a4) through estrogen receptor β and the MAPK/ERK signaling pathway. [Abstract]

2022 Jun 5;924:174939. PMID: 35398393
Biomolecules

Zearalenone Induces Gap Junction Damage in Ovine Ovarian Granulosa Cells by Upregulating GPR30 and Activating the Oxidative Stress-NLRP3 Inflammasome Axis. [Abstract]

2026 Jun 7;16(6):837. PMID: 42352304
Int J Mol Sci

Estradiol and Raloxifene Protect Ovariectomized Mice from Acute Kidney Injury via G Protein-Coupled Estrogen Receptor-Mediated Nuclear Factor Erythroid 2-Related Factor 2/Heme Oxygenase-1 Activation. [Abstract]

2026 Mar 27;27(7):3070. PMID: 41977254
Int Immunopharmacol

GPER governs the immune infiltration of gastric cancer and activates the NF-κB/ROS/Apoptosis pathway in gastric mucosal epithelium. [Abstract]

2023 Sep:122:110641. PMID: 37487261
J Clin Endocrinol Metab

Organoid Cultures Derived From Patients With Papillary Thyroid Cancer. [Abstract]

2021 Apr 23;106(5):1410-1426. PMID: 33524147
Chem Biol Interact

Benzotriazole ultraviolet stabilizers impair trophoblast function at nanomolar concentrations via GPER signaling: implications for placental health. [Abstract]

2026 Jun 1:432:112055. PMID: 41865781
J Nutr Biochem

Genistein maintains intestinal homeostasis in colitis mice via activating GPR30-Nrf2 signaling pathway. [Abstract]

2025 Nov:145:110036. PMID: 40684867
Chem Biol Interact

Fluornen-9-bisphenol increases Leydig cell proliferation but inhibits maturation in pubertal male rats via interacting with androgen receptor as an antagonist and estrogen receptor α as an agonist. [Abstract]

2022 Aug 25:363:110024. PMID: 35764126
Mediators Inflamm

G Protein-Coupled Receptor 30 Attenuates Neuronal Pyroptosis Induced by Subarachnoid Hemorrhage. [Abstract]

2025 Jul 21:2025:3585885. PMID: 40726812
J Cell Mol Med

17-β-Estradiol Protects Chondrocytes From Senescence and Ameliorates Osteoarthritis Progression via ERα-AKT-FOXO4 Pathway. [Abstract]

2026 Feb;30(3):e71018. PMID: 41677002
Poult Sci

17β-estradiol mediates sex-biased progesterone receptor expression via estrogen receptor α in chicken pituitary. [Abstract]

2025 Dec 5;105(1):106210. PMID: 41380332

G15 purchased from MedChemExpress. Usage Cited in: Poult Sci. 2025 Dec 5;105(1):106210. [Abstract]

Effects of selective receptor agonists (PPT, DPN and G-1) treatment (3 h) on PGR expression, and antagonist (ICI and G15) treatment (3 h) on E2-upregulated PGR expression, in cultured pituitary cells from female chicks.
Front Mol Neurosci

The chronification mechanism of orofacial inflammatory pain: Facilitation by GPER1 and microglia in the rostral ventral medulla. [Abstract]

2023 Jan 6:15:1078309. PMID: 36683848
J Cell Physiol

17β-Estradiol mediates TGFBR3/Smad2/3 signaling to attenuate the fibrosis of TGF-β1-induced bovine endometrial epithelial cells via GPER. [Abstract]

2024 Jan;239(1):166-179. PMID: 37991438
Metab Brain Dis

Genistein-3'-sodium sulfonate suppresses NLRP3-mediated cell pyroptosis after cerebral ischemia. [Abstract]

2025 Jan 14;40(1):99. PMID: 39808354
J Biochem Mol Toxicol

Estrogen Promotes the Proliferation and Migration of Endometrial Cancer Through the GPER-Mediated NOTCH Pathway. [Abstract]

2025 Feb;39(2):e70129. PMID: 39878097
Food Chem Toxicol

The environmental estrogen Bisphenol (A) enhances lung cancer progression in vitro and in vivo in presence of estradiol by targeting PI3k/Akt pathway. [Abstract]

2026 Jun 2:215:116197. PMID: 42235672
Food Chem Toxicol

MEHP promotes breast cancer progression via GPR30-mediated epithelial-mesenchymal transition. [Abstract]

2026 Jun:212:116049. PMID: 41780712
Neurosci Res

Ginsenoside Rb1, a principal effective ingredient of Panax notoginseng, produces pain antihypersensitivity by spinal microglial dynorphin A expression. [Abstract]

2023 Mar:188:75-87. PMID: 36368461
Biol Reprod

G protein-coupled estrogen receptor promotes acrosome reaction via regulation of Ca2+ signaling in mouse sperm. [Abstract]

2022 Oct 11;107(4):1026-1034. PMID: 35774023
Food Chem Toxicol

Bisphenol F blocks Leydig cell maturation and steroidogenesis in pubertal male rats through suppressing androgen receptor signaling and activating G-protein coupled estrogen receptor 1 (GPER1) signaling. [Abstract]

2022 Sep:167:113268. PMID: 35803362
J Steroid Biochem Mol Biol

G protein-coupled estrogen receptor reduces the breast cancer cell survival by regulating the IRE1α/miR-17-5p/TXNIP pathway. [Abstract]

2025 Sep:252:106770. PMID: 40328365
Steroids

Exploration of interaction property between nonylphenol and G protein-coupled receptor 30 based on molecular simulation and biological experiments. [Abstract]

2022 Dec:188:109114. PMID: 36154832
Exp Neurobiol

G protein-coupled Estrogen Receptor Activation Exerts Protective Effects via Modulating Brain and Gut NLRP3 Inflammasome in Parkinson's Disease. [Abstract]

2025 Oct 31;34(5):200-213. PMID: 41152022
J Histotechnol

G protein-coupled receptor 30 activation protects hepatic ischemia-reperfusion injury of liver tissue through inhibiting NLRP3 in the rat model. [Abstract]

2021 Mar;44(1):27-36. PMID: 33210578
J Cardiothorac Surg

GPER1-mediated suppression of acute cellular rejection in murine cervical heart transplantation by estradiol. [Abstract]

2025 Apr 17;20(1):208. PMID: 40247327
Hong Kong Polytechnic University

2025.
Sci Total Environ

Triclocarban and triclosan promote breast cancer progression in vitro and in vivo via activating G protein-coupled estrogen receptor signaling pathways. [Abstract]

2024 Jun 25:931:172782. PMID: 38679099
SSRN

2023 Nov 29.
Research Square Preprint

2023 Jun 16.
Evid Based Complement Alternat Med

Shikonin Mediates Apoptosis through G Protein-Coupled Estrogen Receptor of Ovarian Cancer Cells. [Abstract]

2022 Oct 5:2022:6517732. PMID: 36248433
J Cancer Ther

Breast Cancer MCF-7 Cell Spheroid Culture for Drug Discovery and Development. [Abstract]

2022 Mar;13(3):117-130. PMID: 36311820
J Oncol

GPR30 Activation Promotes the Progression of Gastric Cancer and Plays a Significant Role in the Anti-GC Effect of Huaier. [Abstract]

2022 Jan 19:2022:2410530. PMID: 35096058

Solvant et solubilité

In Vitro:

DMSO : 41.67 mg/mL (112.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7010 mL

13.5048 mL

27.0095 mL

5 mM

0.5402 mL

2.7010 mL

5.4019 mL

10 mM

0.2701 mL

1.3505 mL

2.7010 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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 [Content Brief]

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7010 mL	13.5048 mL	27.0095 mL	67.5238 mL
	5 mM	0.5402 mL	2.7010 mL	5.4019 mL	13.5048 mL
	10 mM	0.2701 mL	1.3505 mL	2.7010 mL	6.7524 mL
	15 mM	0.1801 mL	0.9003 mL	1.8006 mL	4.5016 mL
	20 mM	0.1350 mL	0.6752 mL	1.3505 mL	3.3762 mL
	25 mM	0.1080 mL	0.5402 mL	1.0804 mL	2.7010 mL
	30 mM	0.0900 mL	0.4502 mL	0.9003 mL	2.2508 mL
	40 mM	0.0675 mL	0.3376 mL	0.6752 mL	1.6881 mL
	50 mM	0.0540 mL	0.2701 mL	0.5402 mL	1.3505 mL
	60 mM	0.0450 mL	0.2251 mL	0.4502 mL	1.1254 mL
	80 mM	0.0338 mL	0.1688 mL	0.3376 mL	0.8440 mL
	100 mM	0.0270 mL	0.1350 mL	0.2701 mL	0.6752 mL

Keywords

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G15

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) G15

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR

Activité biologique

Chemical Information

Publications (42)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

G15

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) G15

Voir tous les produits spécifiques à Isoform Estrogen Receptor/ERR

Activité biologique

Chemical Information

Publications (42)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

G15 Related Classifications

HY-103449 Related Classifications