计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
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。A disruptor of microtubule function and HIF-1 inhibitor
最大吸收波长:286(EtOH) nm
Information
2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinoge
In vitro
2-Methoxyestradiol exhibits the inhibitory activity of cellular proliferation in a breast carcinoma cell line MDA-MB-435 and an ovarian carcinoma cell line SK-OV-3 with IC50 of 1.38 μM and 1.79 μM, respectively. Furthermore, 2-Methoxyestradiol also inhibits cellular microtubule depolymerization in rat aortic smooth muscle A-10 cells with EC50 of 7.5 μM. 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. A recent study shows that 2-Methoxyestradiol (0.5 μM), blocks TGF-β3-induced expression of collagen (Col) type I(αI), Col III(αI), plasminogen activator inhibitor (PAI) 1, connective tissue growth factor (CTGF), and α-smooth muscle actin (α-SMA). Moreover, 2-Methoxyestradiol ameliorates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibits TGF-β3-induced activation of the PI3K/Akt/mTOR pathway.
In vivo
In a 9L rat glioma (9L-V6R) rat model, 2-Methoxyestradiol significantly decreases HIF-1 activity and inhibits the tumor growth in a dose-dependent manner by 4-fold reduction for 60 mg/kg/day, and 23-fold reduction for 600 mg/kg/day, respectively.
Cell Data
cell lines:
Concentrations:0-20 μM
Incubation Time:48 hours
Powder Purity:≥99%
H301: 吞咽会中毒
H311: 皮肤接触有毒
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H331: 吸入会中毒
H335: 可能引起呼吸道刺激
H350: 可能导致癌症
H360: 可能损害生育力或未出生的孩子
H372: 通过长时间或反复暴露对器官造成损害
H410: 对水生生物有剧毒并具有长期持续影响
| 1. Dingyou Wang, Yuke Ji, Rui Wang, Ke Cheng, Liang Liu, Na Wu, Qing Tang, Xu Zheng, Junxia Li, Zhilong Zhu, Qinghua Wang, Xueyan Zhang, Runbo Li, Jinjin Pan, Zheng Sui, Yuhui Yuan. (2022) Lycopene Ameliorates Hypoxic Pulmonary Hypertension via Suppression of Oxidative Stress. Oxidative Medicine and Cellular Longevity, [10.1155/2022/9179427] |
| 2. Xu Zheng, Jina Zhao, Xiaoqin Jia, Jinjin Pan, Shuo Xu, Dingyou Wang, Junxia Li, Yuke Ji, Zhilong Zhu, Muhammad Hasnain, Zheng Sui, Rui Wang, Yuhui Yuan. (2025) Fucoxanthin Ameliorates Vascular Remodeling via Attenuating Oxidative Stress in Hypoxic Pulmonary Hypertension Rats. JOURNAL OF NUTRITIONAL BIOCHEMISTRY, [PMID:40513841] [10.1016/j.jnutbio.2025.110002] |