2-Methoxyestradiol (2-MeOE2) - Moligand™, 10mM in DMSO , Agonist of GPER, CAS No.362-07-2, Agonist of GPER

CAS: 362-07-2 Cat. No.: M407862 Molecular Weight: 302.41 EC Number: 636-846-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NSC 659853, 2-ME2 | (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinoge
In vitro

2-Methoxyestradiol exhibits the inhibitory activity of cellular proliferation in a breast carcinoma cell line MDA-MB-435 and an ovarian carcinoma cell line SK-OV-3 with IC50 of 1.38 μM and 1.79 μM, respectively. Furthermore, 2-Methoxyestradiol also inhibits cellular microtubule depolymerization in rat aortic smooth muscle A-10 cells with EC50 of 7.5 μM. 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. A recent study shows that 2-Methoxyestradiol (0.5 μM), blocks TGF-β3-induced expression of collagen (Col) type I(αI), Col III(αI), plasminogen activator inhibitor (PAI) 1, connective tissue growth factor (CTGF), and α-smooth muscle actin (α-SMA). Moreover, 2-Methoxyestradiol ameliorates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibits TGF-β3-induced activation of the PI3K/Akt/mTOR pathway.

In vivo

In a 9L rat glioma (9L-V6R) rat model, 2-Methoxyestradiol significantly decreases HIF-1 activity and inhibits the tumor growth in a dose-dependent manner by 4-fold reduction for 60 mg/kg/day, and 23-fold reduction for 600 mg/kg/day, respectively.
Cell Data

cell lines：

Concentrations：0-20 μM

Incubation Time：48 hours

Powder Purity:≥99%

Specifications

Synonyms

NSC 659853, 2-ME2 | (8R, 9S, 13S, 14S, 17S)-2-methoxy-13-methyl-7, 8, 9, 11, 12, 13, 14, 15, 16, 17-decahydro-6H-cyclopenta[a]phenanthrene-3, 17-diol

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

AGONIST

Mechanism of action

Agonist of GPER

Names and Identifiers

• Isomeric SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=C(C=C34)OC)O
• WGK Germany: 3
• RTECS: KG7537500
• Molecular Weight: 302.41
• Reaxy-Rn: 1992189
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=1992189&ln=

Associated Targets(Human)

SHBG Tchem Sex hormone-binding globulin (1 Activities)

Discover Target: SHBG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Specific Rotation[α]: 107° (C=0.5,THF)
• Melt Point(°C): 187 °C

References

1. Dingyou Wang, Yuke Ji, Rui Wang, Ke Cheng, Liang Liu, Na Wu, Qing Tang, Xu Zheng, Junxia Li, Zhilong Zhu, Qinghua Wang, Xueyan Zhang, Runbo Li, Jinjin Pan, Zheng Sui, Yuhui Yuan.  (2022)  Lycopene Ameliorates Hypoxic Pulmonary Hypertension via Suppression of Oxidative Stress.  Oxidative Medicine and Cellular Longevity,      [PMID:] [10.1155/2022/9179427]

2. Xu Zheng, Jina Zhao, Xiaoqin Jia, Jinjin Pan, Shuo Xu, Dingyou Wang, Junxia Li, Yuke Ji, Zhilong Zhu, Muhammad Hasnain, Zheng Sui, Rui Wang, Yuhui Yuan.  (2025)  Fucoxanthin Ameliorates Vascular Remodeling via Attenuating Oxidative Stress in Hypoxic Pulmonary Hypertension Rats.  JOURNAL OF NUTRITIONAL BIOCHEMISTRY,      [PMID:40513841] [10.1016/j.jnutbio.2025.110002]