| 2,4-DPDcell permeable, competitive inhibitor of HIF-PH |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 41438-38-4 | SDF | Download SDF |
| Synonyms | 2,4-Diethylpyridine dicarboxylate | ||
| Chemical Name | 2,4-pyridinedicarboxylic acid, diethyl ester | ||
| Canonical SMILES | O=C(OCC)C1=NC=CC(C(OCC)=O)=C1 | ||
| Formula | C11H13NO4 | M.Wt | 223.2 |
| Solubility | ≤50mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A solution in ethanol | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
