Home Angiogenesis HIF inhibitor - Microtubule Associated modulator - Apoptosis related activator - Autophagy activator 2-Methoxyestradiol (2-MeOE2) For research use only.

2-Methoxyestradiol (2-MeOE2)

Synonyms: NSC 659853, 2-ME2

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.

2-Methoxyestradiol (2-MeOE2) Chemical Structure

2-Methoxyestradiol (2-MeOE2) Chemical Structure

CAS No. 362-07-2

Purity & Quality Control

2-Methoxyestradiol (2-MeOE2) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HOP-62 cytotoxicity assay ~100 μM GI50=0.70 μM 9240348
HCT-116 cytotoxicity assay ~100 μM GI50=0.47 μM 9240348
SF-539 cytotoxicity assay ~100 μM GI50=0.32 μM 9240348
UACC-62 cytotoxicity assay ~100 μM GI50=0.36 μM 9240348
OVCAR-3 cytotoxicity assay ~100 μM GI50=0.21 μM 9240348
SN12C cytotoxicity assay ~100 μM GI50=0.95 μM 9240348
DU-145 cytotoxicity assay ~100 μM GI50=1.8 μM 9240348
MDA-MB-435 cytotoxicity assay ~100 μM GI50=0.08 μM 9240348
LNCaP Growth inhibitory assay ~50 μM IC50=0.5 μM 16650989
DU145 Growth inhibitory assay GI50=1.22 μM 17696419
MDA-MB-23  Growth inhibitory assay GI50=0.94 μM 17696419
MCF7 Growth inhibitory assay GI50=2.35 μM 17696419
U87-MG Growth inhibitory assay IC50=8.54 μM 19762246
PC3 Growth inhibitory assay IC50=2.65 μM 19762246
HUVEC Growth inhibitory assay IC50=0.84 μM 19762246
U937 Growth inhibitory assay IC50=2.91 μM 20334421
SK-OV-3 Function assay circumvents Pgp-mediated drug resistance with EC50 of 867 nM 20973488
SK-OV-3 MDR-1-6/6 Function assay circumvents Pgp-mediated drug resistance with EC50 of 2268 nM 20973488
HeLa Function assay inhibitsβIII-tubulin on drug sensitivity 20973488
HUVEC Function assay shows antiangiogenic activity 21928794
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Biological Activity

Description 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.
Targets
HIF-2α [1]
(Rat aortic smooth muscle A-10 cells)		 Microtubule Associated [1]
(Cell-free assay)		 HIF-1α [3]
(MDA-MB-231 cells)
In vitro
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. [1] 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. [2] In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. [3] 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. [4]
Kinase Assay Microtubule depolymerizing activity
The effects of 2-Methoxyestradiol on cellular microtubule depolymerization are determined by indirect immunofluorescence techniques in rat aortic smooth muscle A-10 cells. Microtubules are visualized using a β-tubulin antibody. Three viewers determines the percent microtubule loss for each treatment concentration. The data are averaged and plotted as percent microtubule loss versus drug concentration and the EC50s for microtubule depolymerization calculated from the log dose–response curves.
Cell Research Cell lines MDA-MB-435 and SK-OV-3
Concentrations 0-20 μM
Incubation Time 48 hours
Method

The sulforhodamine B (SRB) assay is used to evaluate the antiproliferative activity of 2-Methoxyestradiol in the MDA-MB-435 and SK-OV-3 cell lines. Cells a plated into 96-well plates and allowed to grow and attach for 24 hours followed by addition of 2-Methoxyestradiol or vehicle controls. The cells are incubated with drugs for 48 hours and then the cellular protein is fixed, stained, and concentration determined by absorbance at 560 nm. Log dose–response curves are constructed for each experiment and the IC50 for inhibition of proliferation determined.
In Vivo
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. [5]
Animal Research Animal Models 9L-V6R cells are injected into the brains of Fischer 344 rats
Dosages ≤600 mg/kg
Administration Administered via i.p.

Chemical Information & Solubility

Molecular Weight 302.41 Formula

C19H26O3
CAS No. 362-07-2 SDF Download 2-Methoxyestradiol (2-MeOE2) SDF
Smiles CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (198.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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