IOX1 is a cell-permeable broad-spectrum inhibitor of most 2OG oxygenases.  It inhibits histone demethylase JMJD3, JMJD1A, JMJD2A, JMJD2E, JMJD2C and UTX with IC₅₀ at 0.12, 0.17, 0.2, 0.3, 0.6 and 1 μM respectively. IOX1 inhibits JMJD2A-mediated H3K9me3 demethylation in HeLa cells.

How to Use:

• In vitro:  IOX1 was used at 10-300 µM final concentration in various in vitro assays.
• In vivo:  n/a 

Reference:

• 1. King ON, et al. Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors. (2010) PLoS One. 5(11):e15535.
• 2. Schiller R, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. (2014) ChemMedChem. 9(3):566-71.
• 3. http:// http://www.thesgc.org/chemical-probes/IOX1

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