G15

Catalog No.S6651 Batch:S665101

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Technical Data

Formula

C19H16BrNO2
Molecular Weight 370.24 CAS No. 1161002-05-6
Solubility (25°C)* In vitro DMSO 74 mg/mL (199.87 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
Targets
GPER [1]
In vitro

G15 inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines. G15 inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines.[1]
In vivo

G15 decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    A549, H1793 cell lines

  • Concentrations

    0.1 μM, 1 μM, 10 μM

  • Incubation Time

    2 days

  • Method

    To investigate the effects of G15 on tumor cell proliferation, the growth of A549 and H1793 cells is examined using the CCK-8 assay after administering 1, 10, and 100 nM selective agonist G1 and 1, 10, and 100 nM E2, and 10 nM E2 with 0.1, 1, and 10 μM Ful and 10 nM G1 with 0.1, 1, and 10 μM G15.

Selleck's G15 has been cited by 6 publications

YAP-mediated GPER signaling impedes proliferation and survival of prostate epithelium in benign prostatic hyperplasia [ iScience, 2024, 27(3):109125] PubMed: 38420594
GPER/PKA-Dependent Enhancement of Hormone-Sensitive Lipase Phosphorylation in 3T3-L1 Adipocytes by Piceatannol [ Nutrients, 2023, 16(1)38] PubMed: 38201867
Icariin inhibits hypertrophy by regulation of GPER1 and CaMKII/HDAC4/MEF2C signaling crosstalk in ovariectomized mice [ Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110728] PubMed: 37739049
Casein kinase 1 controls the shuttling of epidermal growth factor receptor and estrogen receptor in endometrial carcinoma induced by breast cancer hormonal therapy: Relevance of GPER1/Src [ Cell Signal, 2023, 108:110733] PubMed: 37257767
Effects of neural-derived estradiol on actin polymerization and synaptic plasticity-related proteins in prefrontal and hippocampal cells of mice [ Steroids, 2021, 177:108935] PubMed: 34715132
Promotion effects of mono-2-ethyhexyl phthalate (MEHP) on migration and invasion of human melanoma cells via activation of TGF-β signals. [ Cell Biochem Funct, 2020, 38(1):38-46] PubMed: 31667872

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.