IOX2

IOX2 : Inhibitor of EGLN1

Structure

Information

  • EGLN1
  • Inhibitor
  • 1 µM

In Vitro Validations

Uniprot ID: Q9GZT9
Target Class: Enzyme
Target SubClass: Hydrolase
Potency: IC50
Potency Value: 22 nM
Potency Assay: In vitro Demethylation Assay (alphascreen)
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Egl nine homolog 1, C1orf12, EGLN1, EGLN1_HUMAN, P ...

DOI Reference: 10.1021/cb400088q

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): IOX2 was profiled against a panel of human histone Nε-methyl lysine demethylase 2OG-oxygenases in an AlphaScreen assay to determine selectivity. IOX2 was found to be inactive against a panel of 55 receptors and ion channels (CEREP panel) at 10µM.
Potency assay, off target (cells): Selective inhibition of IOX2 in human cell lines. Selectivity of the tested inhibitors for HIF-1α prolyl- over asparaginyl- hydroxylation in RCC4 after 6h of treatment. Upregulation of HIF-1α by inhibitors in various cell types (after 6h of treatment)
Potency assay (off target): IOX2 was tested against a panel of other human 2OG oxygenases focusing on histone Nε-methyl lysine demethylases (KDMs). The results indicate that IOX2 is at least 2–5000 fold selective, as judged by IC50 values, for PHD2 over the KDMs and FIH. DOI: 10.1021/cb400088q
I have extra information to add

SERP ratings and comments


No SERP comments found for IOX2