2-methoxyestradiol 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.
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HazMat fee for 500 gram (Estimated)
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Limited Quantity
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Inaccessible (Haz class 6.1), Domestic
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The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1α and HIF-2α are structurally similar and can be degraded rapidly under normoxia. 2-Methoxyestradiol can inhibit HIF-1α and HIF-2α expression, as well as depolymerize microtubules. Treatment with 2-Methoxyestradiol (5 - 100 μM) for 16h can reduce expression of HIF-1α dose-dependently in PC-3 and MDA-MB-231 cells, accompanied with the reduced activity of HIF-1 and the expression of its target protein, VEGF, and without effect on HIF-1α mRNA levels or rate of protein degradation. Treatment with 2-Methoxyestradiol (10 - 100 μM) overnight can depolymerize microtubules and impair nuclear accumulation of HIF-1α in PC-3 cells under hypoxia. Daily oral administration of 2-Methoxyestradiol, 150 mg/kg, for 33 days suppressed tumor growth and angiogenesis, as well as depolymerized microtubules in breast cancer orthotopic models. The inhibition of HIF-2α expression and microtubule-depolymerization by 2-Methoxyestradiol can also be observed in endothelial cells[1].
作用机制
2-Methoxyestradiol inhibits the expression, nuclear accumulation and transcriptional activity of HIF-1α[1]. However, the accurate mechanism of action is unknown now.
2-Methoxyestradiol 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
DU145
Growth inhibitory assay
GI50=1.22 μM
17696419
DU-145
~100 μM
cytotoxicity assay
GI50=1.8 μM
9240348
HCT-116
~100 μM
cytotoxicity assay
GI50=0.47 μM
9240348
HeLa
Function assay
inhibitsβIII-tubulin on drug sensitivity
20973488
2-Methoxyestradiol 动物研究
Dose
Rat: min = 0.1 mg/kg, max = 75 mg/kg[2] (p.o.); min = 60 mg/kg, max = 600 mg/kg[3] (i.p.)
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