Potent

IOX2 – 5 mg

Brand:
Cayman
CAS:
931398-72-0
Storage:
-20
UN-No:
Non-Hazardous - /

Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for 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 cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.{21056,21057} IOX2 potently inhibits PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM).{21058} IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.{21058} See the Structural Genomics Consortium (SGC) website for more information.  

 

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SKU: 11573 - 5 mg Category:

Description

Potent, cell permeable inhibitor of PHD2 (IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 μM); inhibits HIF-1α hydroxylation in RCC4 cells at 50 μM

Formal name: N-[[1,2-dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]-glycine

Synonyms: 

Molecular weight: 352.3

CAS: 931398-72-0

Purity: ≥98%

Formulation: A crystalline solid

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

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