产品描述
| 溶解性 | Soluble in DMSO (10 mg/mL), ethanol (10 mg/mL), chloroform, ethanol (1 mg/ml), and 1:1DMF:PBS(pH7.2) (0.5 mg/ml). Insoluble in water. |
| 应用 | A disruptor of microtubule function and HIF-1 inhibitor |
| 产品介绍 | 2-Methoxyestradiol (2-MeOE2)使微管解聚，且抑制HIF-1α核积累和HIF转录活性。Phase 2。 |
| 备注 | 2-Methoxyestradiol depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2. |
| 生化机理 | 2-methoxyestradiol (2ME2) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.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-1α itself. 2-Methoxyestradiol has been shown to induce apoptosis through activation of the p53 pathway through either activation of p38 and NF-κ |
| 别名 | 2-MeOE2;2-甲氧基-β-雌二醇;2-甲氧基雌二醇;2-ME2;(8R,9S,13S,14S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol;2-Methoxy-β-estradiol |
