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Daminozide is a potent and selective small molecule inhibitor of the KDM2/7 family of human JmjC histone demethylases. It inhibits KDM2A at IC₅₀?~1.5 μM, PHF8 at IC₅₀?~0.55 μM, and KIAA1718 at IC50 ~2.1 μM. It has at least 60-fold selectivity as an inhibitor of the KDM2/7 subfamily over the other demethylase subfamily members such as KDM3A, KDM4E, KDM5C and KDM6B, and exhibits no inhibition even at 1 mM for PHD2, FIH, and BBOX1 (all of which are important 2OG oxygenases). The X-ray co-crystal structures revealed the daminozide’s inhibition mode: it binds in the 2OG binding pocket and chelates to the active site metal via its acylhydrazide carbonyl and dimethylamino groups. The selectivity of daminozide for the KDM2/7 subfamily could, at least in part, arise from a “snug fit” obtained via binding in the position trans to His247 wherein its two methyl groups are accommodated in a tight hydrophobic pocket (formed by Val255, Ile313, and Tyr257), which is conserved in the KDM2/7subfamily. Given the link between JmjC enzymes and diseases (such as cancer, metabolic disease, neurological disease, and inflammation), further studies on the biological effects of daminozide is of great interest.

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How to Use:

• In vitro:? Daminozide was used at 10-20 μM final concentration in vitro and in cellular assays.
• In vivo:?n/a

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Reference:?

• 1. Rose NR, et al. Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases (2012) J Med Chem. 55(14):6639-43.?

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