2,4-DPD

A cell permeable, competitive inhibitor of HIF-PH

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货号: ajci16632
CAS: 41438-38-4
别名: 2,4-吡啶二甲酸乙酯,2,4-Diethylpyridine dicarboxylate
分子式: C11H13NO4
分子量: 223.2
纯度: >98%
溶解度: ≤50mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

2,4-DPD is a cell permeable, competitive inhibitor of the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH) [1].

Hypoxia-inducible factor (HIF) is a transcription factor with a key role in cellular responses to hypoxia in a variety of organisms. The HIF system plays an important role in angiogenesis, erythropoiesis, energy utilization, glucose/energy metabolism, tumour development, and ischaemic/hypoxic disease. Genetic or pharmacological inactivation of the HIF hydroxylases results in a constitutive activation of the HIF pathway with little or even absent regulation by oxygen remaining. The oxygen-sensing enzyme HIF-α prolyl hydroxylase catalyzes hydroxylation of specific prolyl and asparaginyl residues in the regulatory HIF-α subunits [2].

Exposure to 2,4-DPD limited prolyl 4-hydroxylase activity in C. elegans., where their esters are hydrolyzed to form competitors of a -ketoglutarate. 2,4-DPD showed dramatic effects among the progeny. When exposed to a high level of 2,4-DPD (2.7 mM), all progeny died regardless of genotype of C. elegans. The dead embryos arrested at the twofold stage [1].

参考文献:
[1] Friedman L, Higgin J J, Moulder G, et al.? Prolyl 4-hydroxylase is required for viability and morphogenesis in Caenorhabditis elegans[J]. Proceedings of the National Academy of Sciences, 2000, 97(9): 4736-4741.
[2] Schofield C J, Ratcliffe P J.? Signalling hypoxia by HIF hydroxylases[J]. Biochemical and biophysical research communications, 2005, 338(1): 617-626.