2 - methoxy estradiol

Quick Detail:

Product name: 2 - methoxy estradiol

Minor: C19H26O3

Content: 98%

Packing: 1 kg aluminum foil bag

usage: steroid raw materials 

Description:

     2-Methoxyestradiol is an endogenous estrogen metabolite with low affinity for the estrogen receptor but which disrupts microtubule function. 2-Methoxyestradiol is formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol. 2-Methoxyestradiol is a derivative of an oestrogenic steroidal hormone and has demonstrated:. potent inhibition of endothelial cell proliferation and migration and inhibition of bFGF and VEGF-induced corneal neovascularization in mice In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF mediated transcriptional activation of target genes without affecting the transcription of HIF-1 pseudo itself. 2-Methoxyestradiol has been shown to induce apoptosis through activation of the p53 pathway through either activation of p38 and NF-B or JNK and AP-1 both leading to Bcl-2 phsophorylation. In addition the compound has also been observed to upregulate death receptor 5 and bind to tubulins.

Applications:

     2-Methoxyestradiol exhibits potent apoptotic activity against rapidly growing tumor cells. It also possesses antiangiogenic activity through a direct apoptotic effect on endothelial cells. Other molecular mechanisms, including microtubule stabilization by inhibition of the colchicine-binding site, have been reported. The exact mechanism of action of 2-methoxyestradiol is still unclear, but it has been shown to be effective in preventing tumor growth in a variety of cell lines. 2-Methoxyestradiol also possesses cardioprotective activity by inhibiting vascular smooth muscle cell growth in arteries. It has a lower binding affinity for estrogen receptor alpha compared with that of estradiol, and its affinity for estrogen receptor beta is even lower than that of estrogen receptor alpha, thus it has minimal estrogenic activity. 2-Methoxyestradiol is distinct because of its inability to engage estrogen receptors as an agonist, and its unique antiproliferative and apoptotic activities are mediated independently of estrogen receptors alpha and beta.

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