2-Methoxyestradiol (2-MeOE2)
Catalog No.S1233 Synonyms: NSC 659853

Molecular Weight(MW): 302.41
2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.
3 Customer Reviews
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The knockdown of Set7 by Set7-shRNA-2 in RCC4 cells increased GST expression, but this effect was not evident when HIF-2 activity was inhibited by addition of 2ME2 (50 ng/µl,18 h), as revealed by semi-quantitative real-time PCR assays.
Nucleic Acids Res, 2015, 43(10): 5081-98 . 2-Methoxyestradiol (2-MeOE2) purchased from Selleck.
Purity & Quality Control
Choose Selective HIF Inhibitors
Biological Activity
Description | 2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Targets |
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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] |
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Cell Data |
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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] |
Protocol
Kinase Assay:[1] |
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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. |
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Cell Research:[1] |
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Animal Research:[5] |
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Solubility (25°C)
In vitro | DMSO | 60 mg/mL (198.4 mM) |
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Water | Insoluble | |
Ethanol | Insoluble | |
In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+corn oil For best results, use promptly after mixing. |
5mg/mL |
* 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.
Chemical Information
Molecular Weight | 302.41 |
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Formula | C19H26O3 |
CAS No. | 362-07-2 |
Storage | powder |
in solvent | |
Synonyms | NSC 659853 |
Bio Calculators
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