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2,4-DPD

 
Catalog No.
C4887
HIF-PH竞争性抑制剂,细胞通透性
组合的产品项目
规格价格库存 数量
50mg (solution)
¥ 1,516.00
Ship with 10-15 days
100mg (solution)
¥ 2,654.00
Ship with 10-15 days

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A

背景

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].

References:
[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.

化学属性

Physical AppearanceA solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
StorageStore at -20°C
M.Wt223.2
Cas No.41438-38-4
FormulaC11H13NO4
Synonyms2,4-Diethylpyridine dicarboxylate
Solubility≤50mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name2,4-pyridinedicarboxylic acid, diethyl ester
SDFDownload SDF
Canonical SMILESO=C(OCC)C1=NC=CC(C(OCC)=O)=C1
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质量控制

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批次:

化学结构

2,4-DPD