DMOG
别名: Dimethyloxalylglycine
DMOG (Dimethyloxalylglycine)是α-酮戊二酸辅助因子的拮抗剂和HIF prolylhydroxylase的抑制剂，它使HIF-1α蛋白在核内稳定并积累，是HIF-1α的激动剂。DMOG 可增加自噬。
DMOG Chemical Structure
CAS: 89464-63-1
客户使用Selleck的DMOG发表文献40篇
产品质控
相关信号通路图
Hydroxylase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | DMOG (Dimethyloxalylglycine)是α-酮戊二酸辅助因子的拮抗剂和HIF prolylhydroxylase的抑制剂，它使HIF-1α蛋白在核内稳定并积累，是HIF-1α的激动剂。DMOG 可增加自噬。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | DMOG在微粒体系统中仅有很低的活性，但在完整细胞中可强烈抑制羟基脯胺酸合成。[1]在HPASMC中，DMOG通过抑制脯氨酰羟化酶降低FGF-2诱导的组织和cyclin A表达。[3] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | VSMC细胞 | ||
| 浓度 | ~100 μM | |||
| 孵育时间 | 72-96 小时 | |||
| 方法 | 为分析DNA合成作为细胞增殖的指数，VSMC细胞以5000个每平方厘米的密度接种在48孔板培养基中，孵育过夜，除去血清（1%FCS）处理24小时。复制的孔板储存−70°C 作为基线（第0天）细胞计数，含有或者不含有生长因子的新鲜培养基加入孔板中，在20%或5%的氧气中孵育72-96小时。第0，3，4天，通过在含有荧光染料的缓冲液中裂解细胞测定细胞数，其自身具有很弱的荧光性，但与DNA或RNA结合时会增强荧光。细胞数目的定量是通过比较样品的荧光与已知细胞数目的标准曲线比较来测定的。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | HIF-1α p-CHK1 / CHK1 / p-p53 / p53 / p-CHK2 / CHK2 / p-ATM / ATM WNT11 / HIF-2α |
|
29555474 | |
| Immunofluorescence | HIF1α |
|
28955984 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
在小鼠局部缺血的骨骼肌中，DMOG抑制內源性HIF失活，诱导血管新生。[2]在高血脂症大鼠体内，通过DMOG上调的缺氧诱导因子1a能够增强缺血后处理的心脏保护作用。[4] |
|
|---|---|---|
| 动物实验 | Animal Models | 小鼠(C57Bl6) |
| Dosages | 8毫克在0.5毫升生理盐水中 | |
| Administration | 腹腔注射 | |
化学信息&溶解度
| 分子量 | 175.14 | 分子式 | C6H9NO5 |
| CAS号 | 89464-63-1 | SDF | Download DMOG SDF |
| 密度 | 1.246 g/mL | ||
| Smiles | COC(=O)CNC(=O)C(=O)OC | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 35 mg/mL ( (199.84 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 35 mg/mL Ethanol : 35 mg/mL |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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