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別名: Dimethyloxalylglycine
DMOG (Dimethyloxalylglycine)是α-酮戊二酸輔助因子的拮抗劑和HIF prolylhydroxylase的抑制劑,它使HIF-1α蛋白在核內(nèi)穩(wěn)定并積累,是HIF-1α的激動劑。DMOG 可增加自噬。在溶液中不穩(wěn)定,請現(xiàn)配現(xiàn)用!
DMOG Chemical Structure
CAS: 89464-63-1
相關靶點 | DBH KMO TPH | 點擊展開 |
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相關產(chǎn)品 | Ro 61-8048 Meldonium 4-Chloro-DL-phenylalanine | 點擊展開 |
相關化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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human 293T cells? | Function assay | 2.5 mM | Inhibition of JMJD2-mediated H3K36 demethylation in human 293T cells at 2.5 mM | 19359167 | |
human SW982 cell | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=33.7007 μM | SANGER | ||
human OPM-2 cell | Growth inhibition assay | Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=28.8227 μM | SANGER | ||
human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=28.4579 μM | SANGER | ||
human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=26.5502 μM | SANGER | ||
human COR-L105 cell | Growth inhibition assay | Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=26.4436 μM | SANGER | ||
human LC-2-ad cell | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=24.5573 μM | SANGER | ||
human YT cell | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=23.3984 μM | SANGER | ||
human KYSE-410 cell | Growth inhibition assay | Inhibition of human KYSE-410 cell growth in a cell viability assay, IC50=20.8197 μM | SANGER | ||
human CAL-39 cell | Growth inhibition assay | Inhibition of human CAL-39 cell growth in a cell viability assay, IC50=19.3277 μM | SANGER | ||
human DMS-273 cell | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=15.965 μM | SANGER | ||
human BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=15.9423 μM | SANGER | ||
human A3-KAW cell | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=15.8174 μM | SANGER | ||
human U-698-M cell | Growth inhibition assay | Inhibition of human U-698-M cell growth in a cell viability assay, IC50=13.3306 μM | SANGER | ||
human KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=11.2557 μM | SANGER | ||
human LOUCY cell | Growth inhibition assay | Inhibition of human LOUCY cell growth in a cell viability assay, IC50=10.3493 μM | SANGER | ||
human LB996-RCC cell | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=5.6877 μM | SANGER | ||
human SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=4.57946 μM | SANGER | ||
human HH cell | Growth inhibition assay | Inhibition of human HH cell growth in a cell viability assay, IC50=34.0235 μM | SANGER | ||
human RS4-11 cell | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=34.1806 μM | SANGER | ||
human BEN cell | Growth inhibition assay | Inhibition of human BEN cell growth in a cell viability assay, IC50=36.8187 μM | SANGER | ||
human CCRF-CEM cell | Growth inhibition assay | Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=37.7729 μM | SANGER | ||
human EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=39.0481 μM | SANGER | ||
human NCI-H2228 cell | Growth inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=42.818 μM | SANGER | ||
human KE-37 cell | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=43.2915 μM | SANGER | ||
human A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=45.0364 μM | SANGER | ||
human MZ1-PC cell | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=45.9888 μM | SANGER | ||
human MLMA cell | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50=46.3292 μM | SANGER | ||
human EB-3 cell | Growth inhibition assay | Inhibition of human EB-3 cell growth in a cell viability assay, IC50=49.5792 μM | SANGER | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | DMOG (Dimethyloxalylglycine)是α-酮戊二酸輔助因子的拮抗劑和HIF prolylhydroxylase的抑制劑,它使HIF-1α蛋白在核內(nèi)穩(wěn)定并積累,是HIF-1α的激動劑。DMOG 可增加自噬。在溶液中不穩(wěn)定,請現(xiàn)配現(xiàn)用! | |
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | DMOG在微粒體系統(tǒng)中僅有很低的活性,但在完整細胞中可強烈抑制羥基脯胺酸合成。[1]在HPASMC中,DMOG通過抑制脯氨酰羥化酶降低FGF-2誘導的組織和cyclin A表達。[3] |
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細胞實驗 | 細胞系 | VSMC細胞 | ||
濃度 | ~100 μM | |||
孵育時間 | 72-96 小時 | |||
方法 | 為分析DNA合成作為細胞增殖的指數(shù),VSMC細胞以5000個每平方厘米的密度接種在48孔板培養(yǎng)基中,孵育過夜,除去血清(1%FCS)處理24小時。復制的孔板儲存−70°C 作為基線(第0天)細胞計數(shù),含有或者不含有生長因子的新鮮培養(yǎng)基加入孔板中,在20%或5%的氧氣中孵育72-96小時。第0,3,4天,通過在含有熒光染料的緩沖液中裂解細胞測定細胞數(shù),其自身具有很弱的熒光性,但與DNA或RNA結(jié)合時會增強熒光。細胞數(shù)目的定量是通過比較樣品的熒光與已知細胞數(shù)目的標準曲線比較來測定的。 |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | HIF-1α p-CHK1 / CHK1 / p-p53 / p53 / p-CHK2 / CHK2 / p-ATM / ATM WNT11 / HIF-2α |
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29555474 | |
Immunofluorescence | HIF1α |
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28955984 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | 在小鼠局部缺血的骨骼肌中,DMOG抑制內(nèi)源性HIF失活,誘導血管新生。[2]在高血脂癥大鼠體內(nèi),通過DMOG上調(diào)的缺氧誘導因子1a能夠增強缺血后處理的心臟保護作用。[4] |
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動物實驗 | Animal Models | 小鼠(C57Bl6) |
Dosages | 8毫克在0.5毫升生理鹽水中 | |
Administration | 腹腔注射 |
分子量 | 175.14 | 分子式 | C6H9NO5 |
CAS號 | 89464-63-1 | SDF | Download DMOG SDF |
密度 | 1.246 g/mL | ||
Smiles | COC(=O)CNC(=O)C(=O)OC | ||
儲存條件(自收到貨起) | 3年 -20°C 粉狀 | 此產(chǎn)品性質(zhì)不穩(wěn)定,需現(xiàn)配現(xiàn)用!建議您購買分裝規(guī)格,或者在收到貨后進行分裝。 |
體外溶解度 |
DMSO : 35 mg/mL ( (199.84 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : 35 mg/mL (199.84 mM) Ethanol : 35 mg/mL (199.84 mM) |
摩爾濃度計算器 |
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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