IOX1

IOX1, a chemical probe, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively[1][2]. IOX1 also inhibits ALKBH5[3].

Product Specifications

CAS Number

[5852-78-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/IOX1.html

Purity

99.89

Solubility

DMSO : 13.33 mg/mL (ultrasonic; warming)

Smiles

O=C(C1=C2C=CC=NC2=C(O)C=C1)O

Molecular Formula

C10H7NO3

Molecular Weight

189.17

Precautions

H302, H315, H319, H335

References & Citations

[1]Schiller R, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9 (3) :566-71.|[2]Hu Q, et al. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins. Int J Mol Med. 2016 Jan;37 (1) :189-96.|[3]Li F, et al. A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5. Biomol Screen. 2016 Mar;21 (3) :290-7.|[4]Yuan Deng, et al. Histone demethylase JMJD2D promotes the self-renewal of liver cancer stem-like cells by enhancing EpCAM and Sox9 expression. J Biol Chem