DMOG

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Chemical Structure| 89464-63-1 同义名 : Dimethyloxallyl Glycine; Dimethyloxalylglycine; Dimethyloxaloylglycine
CAS号 : 89464-63-1
货号 : A160647
分子式 : C6H9NO5
纯度 : 98%
分子量 : 175.14
MDL号 : MFCD05865098
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
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
生物活性
靶点

  • PHD1

  • Hydroxylase
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 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
实验方案
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
参考文献

[1]Baader E, Tschank G, et al. Inhibition of prolyl 4-hydroxylase by oxalyl amino acid derivatives in vitro, in isolated microsomes and in embryonic chicken tissues. Biochem J. 1994 Jun 1;300 ( Pt 2):525-30.

[2]Jaakkola P, Mole DR, et al. Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. Science. 2001 Apr 20;292(5516):468-72. Epub 2001 Apr 5.

[3]Hoppe G, Yoon S, et al. Comparative systems pharmacology of HIF stabilization in the prevention of retinopathy of prematurity. Proc Natl Acad Sci U S A. 2016 May 3;113(18):E2516-25.

[4]Cunliffe CJ, Franklin TJ, et al. Novel inhibitors of prolyl 4-hydroxylase. 3. Inhibition by the substrate analogue N-oxaloglycine and its derivatives. J Med Chem. 1992 Jul 10;35(14):2652-8.

[5]Yang N, Wei Y, et al. Genome-wide analysis of DNA methylation during antagonism of DMOG to MnCl2-induced cytotoxicity in the mouse substantia nigra. Sci Rep. 2016 Jul 6;6:28933.

[6]Hams E, Saunders SP, et al. The hydroxylase inhibitor dimethyloxallyl glycine attenuates endotoxic shock via alternative activation of macrophages and IL-10 production by B1 cells. Shock. 2011 Sep;36(3):295-302.