Drug intelligence / Profile preview

IOX2

Development stage
Preclinical
Lead developer
Structural Genomics Consortium
Modality
Small Molecules
Administration
Experimental (in Vitro/in Vivo Research, Not For Clinical Use)
01

Overview

IOX2 is a **potent and selective small molecule inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase-2 (PHD2)** with an IC50 of approximately 21–22 nM and over 100-fold selectivity versus other related enzymes such as FIH and JMJD2 family demethylases. By inhibiting PHD2, IOX2 blocks the oxygen-dependent prolyl hydroxylation of HIF-1α, leading to stabilization and accumulation of HIF-1α protein, mimicking cellular responses to hypoxia. IOX2 is widely used as a **chemical probe** in the study of the hypoxic response, cellular metabolism, oxygen sensing, and HIF pathway biology. It has also demonstrated activity in in vivo models (e.g., zebrafish) and ex vivo/in vitro assays across multiple mammalian cell lines. IOX2 is primarily a research tool and not approved for clinical therapy, but has relevance in anemia, ischemia, wound healing research, and is a target of interest in anti-doping studies due to its capacity to enhance molecular oxygen transport.

Other names
IOX2IOX-2IOX 2(1-benzyl-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbonyl)glycineJICL38JICL-38JICL 38
02

Targets

EGLN1 (Prolyl hydroxylase domain-containing protein 2)

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