货号:A160647 同义名: Dimethyloxallyl Glycine;Dimethyloxalylglycine
DMOG 是一种 HIF-1α 稳定剂,能够抑制 HIF-1α 的降解。DMOG 主要用于缺氧反应、血管生成和癌症的研究。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
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Inaccessible (Haz class 6.1), International | USD 150+ |
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产品名称 | HIF ↓ ↑ | HIF1 ↓ ↑ | PHD1 ↓ ↑ | PHD2 ↓ ↑ | PHD3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
KC7F2 |
+
HIF-1α, IC50: 20 μM |
+
HIF-1α, IC50: 20 μM |
98% | ||||||||||||||||
Lificiguat | ✔ | 99%+ | |||||||||||||||||
BAY 87-2243 | ✔ | 99%+ | |||||||||||||||||
PX-478·2HCl | ✔ | 98%+ | |||||||||||||||||
2-Methoxyestradiol | ✔ | 98% | |||||||||||||||||
CAY10585 |
++
HIF, IC50: 4.4 μM |
BCRP | 97% | ||||||||||||||||
DMOG | ✔ | 98% | |||||||||||||||||
FG 2216 |
++
PHD2, IC50: 3.9 μM |
99%+ | |||||||||||||||||
MK-8617 |
++++
PHD1, IC50: 1 nM |
++++
PHD2, IC50: 1 nM |
++++
PHD3, IC50: 14 nM |
99%+ | |||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | The family of HIF-PH (HIF prolyl hydroxylase) enzymes are the main molecular to regulate HIF activity through hydroxylation at 2 proline residues and cause the degradation of HIF, thus leading to inhibition on accumulation of functional HIF under normoxia. DMOG (Dimethyloxalylglycine) is a prolyl 4-hydroxylase inhibitor with IC50 value of 2 μM (measured by hydroxyproline formation in chicken embryo calvaria) [1]. HIF-1α is strongly induced in Hep3B and U2OS cells exposure to 100 μM or 1000 μM DMOG for 6h under normoxic culture conditions[2]. Administration to newborn pups by i.p. injections at a dose of 200 mg/kg DMOG conferred a protective phenotype in the retinopathy of prematurity (ROP) model[3]. |
作用机制 | DMOG, an analog to 2OG, can inhibit prolyl 4-hydroxylase in a competitive manner[4]. It is the most structurally basic 2OG-derived HIF stabilizer[3]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 293T cells | 2.5 mM | Function assay | Inhibition of JMJD2-mediated H3K36 demethylation in human 293T cells at 2.5 mM | 19359167 | |
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 A4-Fuk cell | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=45.0364 μM | SANGER | ||
human BEN cell | Growth inhibition assay | Inhibition of human BEN cell growth in a cell viability assay, IC50=36.8187 μM | SANGER | ||
Dose | Mice: 8 mg/Mice[5] (i.p.); 20 mg/kg - 100 mg/kg[6] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
5.71mL 1.14mL 0.57mL |
28.55mL 5.71mL 2.85mL |
57.10mL 11.42mL 5.71mL |
CAS号 | 89464-63-1 |
分子式 | C6H9NO5 |
分子量 | 175.139 |
别名 | Dimethyloxallyl Glycine;Dimethyloxalylglycine;Dimethyloxaloylglycine |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(599.52 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 50 mg/mL(285.49 mM),配合低频超声助溶 |
动物实验配方 |