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.
Cited by 6 Publications
2 Customer Reviews
Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.
Oncotarget, 2015, 6(4): 2250-62. 2-Methoxyestradiol (2-MeOE2) purchased from Selleck.
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
Click to view more
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.|
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. |
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.
-  Rao PN, et al. Steroids. 2002, 67(13-14), 1079-1089.
-  Seeger H, et al. J Steroid Biochem Mol Biol. 2003, 84(2-3), 255-257.
-  Mabjeesh NJ, et al. Cancer Cell. 2003, 3(4), 363-375.
|In vitro||DMSO||60 mg/mL (198.4 mM)|
|In vivo||2% DMSO+corn oil||5mg/mL|
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00328497||Completed||Carcinoid Tumor||CASI Pharmaceuticals, Inc.||May 2006||Phase 2|
|NCT00028821||Completed||Refractory Multiple Myeloma|Stage III Multiple Myeloma|Unspecified Adult Solid Tumor, Protocol Specific||National Cancer Institute (NCI)||January 2002||Phase 1|
|NCT00030095||Completed||Unspecified Adult Solid Tumor, Protocol Specific||National Cancer Institute (NCI)||September 2001||Phase 1|
|NCT00592579||Completed||Relapsed Multiple Myeloma|Plateau Phase Multiple Myeloma||CASI Pharmaceuticals, Inc.||March 2001||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.