IOX2

IOX2 : Inhibitor of EGLN1

Structure

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Information

EGLN1

Inhibitor

1 µM

Additional Data

SGC Chemical Probe Collection

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

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