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IOX4

Names

[ CAS No. ]:
1154097-71-8

[ Name ]:
IOX4

[Synonym ]:
2-Methyl-2-propanyl 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

Biological Activity

[Description]:

IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Research Areas >> Neurological Disease

[Target]

IC50: 1.6 nM (PHD2)[1]


[In Vitro]

IOX4 (1-100 μM; 5 hours) determines the EC50s for HIF1α induction are 114 μM, 86 μM and 49.5 μM in MCF-7, Hep3B and U2OS, respectively[1].

[References]

[1]. Chan MC, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. PLoS One. 2015 Jul 6;10(7):e0132004.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
502.2±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H16N6O3

[ Molecular Weight ]:
328.326

[ Flash Point ]:
257.5±32.9 °C

[ Exact Mass ]:
328.128387

[ LogP ]:
0.73

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.673

Related Compounds