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受注：045-509-1970 |
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化学情報
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Synonyms | NSC 659853, 2-ME2 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C19H26O3 |
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| 分子量 | 302.41 | CAS No. | 362-07-2 | |
| Solubility (25°C)* | 体外 | DMSO | 60 mg/mL (198.4 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | 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 carcinogenic cell lines. |
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| 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. [1] 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. [2] In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. [3] 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. [4] |
| 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. [5] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Microtubule depolymerizing activity | |
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| The effects of 2-Methoxyestradiol on cellular microtubule depolymerization are determined by indirect immunofluorescence techniques in rat aortic smooth muscle A-10 cells. Microtubules are visualized using a β-tubulin antibody. Three viewers determines the percent microtubule loss for each treatment concentration. The data are averaged and plotted as percent microtubule loss versus drug concentration and the EC50s for microtubule depolymerization calculated from the log dose–response curves. | ||
| 細胞アッセイ | 細胞株 | MDA-MB-435 and SK-OV-3 |
| 濃度 | 0-20 μM | |
| 反応時間 | 48 hours | |
| 実験の流れ | The sulforhodamine B (SRB) assay is used to evaluate the antiproliferative activity of 2-Methoxyestradiol in the MDA-MB-435 and SK-OV-3 cell lines. Cells a plated into 96-well plates and allowed to grow and attach for 24 hours followed by addition of 2-Methoxyestradiol or vehicle controls. The cells are incubated with drugs for 48 hours and then the cellular protein is fixed, stained, and concentration determined by absorbance at 560 nm. Log dose–response curves are constructed for each experiment and the IC50 for inhibition of proliferation determined. |
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| 動物実験 | 動物モデル | 9L-V6R cells are injected into the brains of Fischer 344 rats |
| 投薬量 | ≤600 mg/kg | |
| 投与方法 | Administered via i.p. | |
参考
カスタマーフィードバック
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Data from [Data independently produced by , , Oncotarget, 2015, 6(4): 2250-62]
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Data from [Data independently produced by , , Nucleic Acids Res, 2015, 43(10): 5081-98 ]
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Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, doi:10.1016/j.mce.2018.05.002]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| HIF-1 inhibition reverses opacity in a rat model of galactose-induced cataract [ PLoS One, 2024, 19(2):e0299145] | PubMed: 38416732 |
| MiR-122-5p regulates the mevalonate pathway by targeting p53 in non-small cell lung cancer [ Cell Death Dis, 2023, 14(4):234] | PubMed: 37005437 |
| Signaling metabolite succinylacetone activates HIF-1α and promotes angiogenesis in GSTZ1-deficient hepatocellular carcinoma [ JCI Insight, 2023, 8(23)e164968] | PubMed: 37906252 |
| Ginkgo biloba extract attenuates cisplatin-induced renal interstitial fibrosis by inhibiting the activation of renal fibroblasts through down-regulating the HIF-1α/STAT3/IL-6 pathway in renal tubular epithelial cells [ Phytomedicine, 2023, 115:154809] | PubMed: 37087791 |
| HIF-1α mediates osteoclast-induced disuse osteoporosis via cytoophidia in the femur of mice [ Bone, 2023, 168:116648] | PubMed: 36563716 |
| MDM2 promotes cancer cell survival through regulating the expression of HIF-1α and pVHL in retinoblastoma [ Pathol Oncol Res, 2023, 29:1610801] | PubMed: 36741966 |
| Blood-nerve barrier enhances chronic postsurgical pain via the HIF-1α/ aquaporin-1 signaling axis [ BMC Anesthesiol, 2023, 23(1):381] | PubMed: 37990154 |
| IL‑4 alleviates CIRI by suppressing autophagy via the HIF‑1α/Bcl‑2/BNIP3 pathway in rats [ Acta Neurobiol Exp (Wars), 2023, 10.55782/ane-2023-2429] | PubMed: 37874193 |
| An E3 ligase TRIM1 promotes colorectal cancer progression via K63-linked ubiquitination and activation of HIF1α [ Research Square, 2023, 10.21203/rs.3.rs-3493586/v1] | PubMed: none |
| Gut microbiota-derived succinate aggravates acute lung injury after intestinal ischemia/reperfusion in mice [ Eur Respir J, 2022, 2200840] | PubMed: 36229053 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。