| Identification | Back Directory | [Name]
IOX4 | [CAS]
1154097-71-8 | [Synonyms]
IOX4
IOX4 NEW
IOX4; IOX-4; IOX 4
PHD2 inhibitor IOX4
t-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
3-Pyridinecarboxylic acid, 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-, 1,1-dimethylethyl ester | [Molecular Formula]
C15H16N6O3 | [MDL Number]
MFCD31691406 | [MOL File]
1154097-71-8.mol | [Molecular Weight]
328.33 |
| Chemical Properties | Back Directory | [Melting point ]
>190° (dec.) | [Boiling point ]
502.2±60.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Refrigerator, Under inert atmosphere | [solubility ]
DMSO (Sparingly, Sonicated), Methanol (Slightly, Sonicated) | [form ]
Solid | [pka]
1.36±0.29(Predicted) | [color ]
Light Beige to Beige |
| Hazard Information | Back Directory | [Description]
IOX4 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 1.6 nM). It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 μM) and inducing HIF-1α and HIF-2α expression in mice. The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier. | [Uses]
IOX4 is a triazole based potent and selective inhibitor of hypoxia-inducible factor (HIF) prolyl-hydroxylase. It induces HIFα in cells of mouse brain. It is useful for studies that aim to validate the upregulation of HIF for treatment of cerebral diseases such as stroke. | [storage]
Store at -20°C |
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