Drug intelligence / Profile preview

IOX1

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, In Vitro (research Use Only)
01

Overview

IOX1 is a synthetic small molecule and a broad-spectrum, cell-permeable inhibitor of 2-oxoglutarate (2OG) oxygenases, particularly the Jumonji C domain-containing histone lysine demethylases (JmjC KDMs). It acts by binding to the active-site Fe(II) and inhibits a range of KDMs, including KDM3, KDM4, KDM6, and KDM2A, with varying potencies. IOX1 modulates epigenetic gene regulation by increasing histone methylation, thereby suppressing the transcription of specific genes such as α-globin in erythroid cells and IL-17 in T cells. It has demonstrated anti-inflammatory, anti-proliferative, and radiosensitizing activities, and is investigated as a tool compound in preclinical models for diseases including β-thalassemia, autoimmune uveitis, sepsis, and cancers such as colorectal cancer and non-small cell lung cancer. IOX1 is not approved for human therapeutic use and currently serves as a research tool for epigenetic and hypoxic signaling studies[1][2][3][4][5][6][7][8].

Other names
8-hydroxy-5-quinolinecarboxylic acid5-carboxy-8HQ
02

Targets

KDM4A (Lysine-specific demethylase 4A)FIH-1 (Factor inhibiting hypoxia-inducible factor 1)KDM6B (Lysine-specific demethylase 6B)KDM2A (Lysine-specific demethylase 2A)KDM3A (Lysine-specific demethylase 3A)

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