2-Methoxyestradiol
Chemical Name: (17β)-2-Methoxyestra-1,3,5(10)-triene-3,17-diol
Purity: ≥99%
Biological Activity
2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent, in vitro and in vivo; acts via an estrogen receptor-independent mechanism. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. Also upregulates death receptor 5 and binds to tubulin, inhibiting its assembly.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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2-MethoxyOE inhibits proliferation and induces apoptosis independently of estrogen receptors α and β.
LaVallee et al.
Cancer Res., 2002;62:3691 -
2-MethoxyOE up-regulates death receptor 5 and induces apoptosis through activation of the extrinsic pathway.
LaVallee et al.
Cancer Res., 2003;63:468 -
Roles of p38 and c-jun NH2-terminal kinase-mediated pathways in 2-methoxyOE-induced p53 induction and apoptosis.
Shimada et al.
Carcinogenesis, 2003;24:1067 -
2-MethoxyOE, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colch. site.
D'Amato et al.
Proc.Natl.Acad.Sci.U.S.A., 1994;91:3964
Product Datasheets
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Citation for 2-Methoxyestradiol
The citations listed below are publications that use Tocris products. Selected citations for 2-Methoxyestradiol include:
1 Citation: Showing 1 - 1
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Hypoxia increases chemoresistance in human medulloblastoma DAOY cells via hypoxia-inducible factor 1α-mediated downregulation of the CYP2B6, CYP3A4 and CYP3A5 enzymes and inhibition of cell proliferation.
Authors: Valencia-Cervantes Et al.
Oncol Rep 2019;41:178
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