1154097-71-8

1154097-71-8 structure

Name: IOX4
Chemical Name: 2-Methyl-2-propanyl 6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]nicotinate
CAS Number: 1154097-71-8
Molecular Formula: C₁₅H₁₆N₆O₃
Molecular Weight: 328.326
Catalog: Signaling Pathways Metabolic Enzyme/Protease HIF/HIF Prolyl-Hydroxylase
Create Date: 2018-06-19 20:16:28
Modify Date: 2024-01-09 17:31:23
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].

Name	2-Methyl-2-propanyl 6-[5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl]nicotinate
Synonyms	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

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.