A selective

IOX4 – 5 mg

Brand:
Cayman
CAS:
1154097-71-8
Storage:
-20
UN-No:
Non-Hazardous - /

Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome.{21056,21057} HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).{29178} 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.{29178} 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.{29178}  

 

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Description

A selective, potent inhibitor of PHD2 (IC50 = 1.6 nM); active in vivo, inhibiting prolyl hydroxylation and increasing HIF1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF1α and HIF2α expression in mice; penetrates the blood-brain barrier to induce HIF expression in the brain

Formal name: 1,1-dimethylethyl ester 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-3-pyridinecarboxylic acid

Synonyms: 

Molecular weight: 328.3

CAS: 1154097-71-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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