Chemical Name: (17β)-2-Methoxyestra-1,3,5(10)-triene-3,17-diol
Biological Activity2-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.
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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.
2-MethoxyOE, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colch. site.
D'Amato et al.
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
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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