Daminozide (1596-84-5) is a selective inhibitor of the KDM2/7 JmjC subfamily of histone demethylases. IC50=1.5, 0.55 and 2.1 μM for KDM2A, PHF8 and KDM7A respectively. Highly selective over other subfamily members (KDM3, KDM4, KDM5 and KDM6) as well as other 2-oxoglutarate oxygenases (FIH, PHD2 and BBOX1), IC50 > 100 μM.1 Decreases tumorsphere formation in human breast cancer cells and acts synergistically with cisplatin in cell killing.2
1) Rose et al. (2012), Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone methylases; J. Med. Chem., 55 6639
2) Chen et al. (2016), Lysine demethylase 2A promotes stemness and angiogenesis of breast cancer by upregulating Jagged1; Oncotarget, 7 27689
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