G36
Based on 1 Customer Validation
G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer.
For research use only. We do not sell to patients.
- Purity: 99.35%
- CAS No.: 1392487-51-2
- Formula: C22H22BrNO2
- Molecular Weight:412.32
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Anti-Cancer Compound Library
HY-L025
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Anti-Breast Cancer Compound Library
HY-L074
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Nuclear Receptor Compound Library
HY-L126
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
G36 (1 µM, 15 minutes) demonstrates inhibitory activity on GPER-mediated ERK activation, effectively blocking E2- and G-1 (HY-107216)-induced ERK activation in SKBr3 cells[1].
G36 (10 µM, 30 minutes) inhibits endothelin-1- and G-1 (HY-107216)-induced contraction of porcine coronary artery rings, indicating its ability to effectively block GPER-mediated coronary artery tension regulation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKBr3 (breast cancer cells expressing only GPER)
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Concentration:1 µM
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Incubation Time:15 minutes
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Result:Inhibited E2- and G-1-induced ERK activation, with no effect on EGF-induced activation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ovariectomy-induced estrogen-dependent uterine proliferation in C57Bl6 mice model[1]
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Dosage:50 µg/kg
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Administration:Subcutaneous injection (s.c.), single dose
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Result:Significantly reduced E2-induced uterine epithelial proliferation by inhibiting cell proliferation.
Chemical Information
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CAS No. 1392487-51-2
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Appearance Solid
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Molecular Weight 412.32
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Formula C22H22BrNO2
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Color White to light yellow
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SMILES
CC(C1=CC2=C(N[C@@H](C3=C(Br)C=C(OCO4)C4=C3)[C@]5([H])[C@@]2([H])C=CC5)C=C1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (121.27 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, Bologa CG, Oprea TI, Yamaguchi Y, Hayashi S, Sklar LA, Hathaway HJ, Arterburn JB, Prossnitz ER. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66. [Content Brief]
[2]. Yu X, et al. The activation of G protein-coupled estrogen receptor induces relaxation via cAMP as well as potentiates contraction via EGFR transactivation in porcine coronary arteries. PLoS One. 2018 Jan 23;13(1):e0191418. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4253 mL | 12.1265 mL | 24.2530 mL | 60.6325 mL |
| 5 mM | 0.4851 mL | 2.4253 mL | 4.8506 mL | 12.1265 mL | |
| 10 mM | 0.2425 mL | 1.2127 mL | 2.4253 mL | 6.0633 mL | |
| 15 mM | 0.1617 mL | 0.8084 mL | 1.6169 mL | 4.0422 mL | |
| 20 mM | 0.1213 mL | 0.6063 mL | 1.2127 mL | 3.0316 mL | |
| 25 mM | 0.0970 mL | 0.4851 mL | 0.9701 mL | 2.4253 mL | |
| 30 mM | 0.0808 mL | 0.4042 mL | 0.8084 mL | 2.0211 mL | |
| 40 mM | 0.0606 mL | 0.3032 mL | 0.6063 mL | 1.5158 mL | |
| 50 mM | 0.0485 mL | 0.2425 mL | 0.4851 mL | 1.2127 mL | |
| 60 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0105 mL | |
| 80 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL | 0.7579 mL | |
| 100 mM | 0.0243 mL | 0.1213 mL | 0.2425 mL | 0.6063 mL |
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