Table 2.
JmjC family inhibitors
| In vitro |
|||||
|---|---|---|---|---|---|
| Name | Where first described | Inhibits | Does not inhibit | Mouse tumor studies | Additional references |
| GSK-J4 | Kruidenier et al. 2012 | KDM5B, KDM5C, KDM6A, KDM6B | KDM4A, KDM4C, KDM4D, KDM4E | Ovarian cancer xenograft | Heinemann et al. 2014; Ntziachristos et al. 2014; Sakaki et al. 2015; Horton et al. 2016 |
| JIB-04 | Wang et al. 2013 | KDM4A, KDM4B, KDM4C, KDM4E, KDM6B | Non-small-cell lung cancer xenograft | Horton et al. 2016 | |
| SD70 | Jin et al. 2014 | KDM4C | Prostate cancer xenograft | ||
| Compound 4 | Chu et al. 2014 | KDM4A, KDM4B | |||
| Compound 6p | Feng et al. 2015 | KDM4A | PHD2 | ||
| Compound 6j | Itoh et al. 2015 | KDM5A | KDM4C, KDM3A | ||
| Compound 13 | Suzuki et al. 2013 | KDM2A, KDM7A, KDM7B | KDM4A, KDM4C, KDM5A, KDM6A | ||
| Compound 3195 | Mannironi et al. 2014 | KDM5A | |||
| Compound B3 | Duan et al. 2015 | KDM4B, KDM4D | KDM4A, KDM4C | ||
| Iridium(III) compound 1 | Liu et al. 2015 | KDM4D | KDM5A, KDM6B, HDAC | ||
| Methylstat | Luo et al. 2011 | KDM4A, KDM4C, KDM4E, KDM6 | PHF8, FIH, LSD1, HDAC | ||
| NCDM-32B | Hamada et al. 2010 | KDM2A, KDM2C | PHD1, PHD2 | ||
| PBIT | Sayegh et al. 2013 | KDM5A, KDM5B, KDM5C | KDM6A, KDM6B | ||
| 2,4 PDCA | Rose et al. 2008 | KDM2A, KDM3A, KDM4A, KDM4C, KDM4D, KDM4E, PHD2, FIH | KDM6A, KDM6B (weak inhibition) | Hopkinson et al. 2013 | |
| Compound 5 | Schiller et al. 2014 | KDM4C, KDM4E | KDM2A, KDM3A, KDM5C, KDM6B, PHD2 | ||
| Compound 7f | Rose et al. 2010 | KDM4A, KDM4E, FIH | PHD2 | ||
| Compound 9 | Woon et al. 2012 | KDM4A | KDM2A, KDM4E, PHF8 | ||
| Compound 15c | Chang et al. 2011 | KDM4E | |||
| Compound 35 | England et al. 2014 | KDM2A | KDM3A, KDM4A, KDM4C, KDM4E, KDM5C, KDM6B | ||
| Compound 42 | Korczynska et al. 2015 | KDM3A, KDM4C, KDM4D, KDM5B | KDM2A, KDM6B, FIH | ||
| Compound 47 | Thalhammer et al. 2011 | KDM4E | PHD2 | ||
| Daminozide | Rose et al. 2012 | KDM2A, KDM7A, PHF8 | KDM3A, KDM4E, KDM5C, KDM6B, FIH, PHD2, BBOX1 | ||
| Disulfiram | Sekirnik et al. 2009 | KDM4A, aldehyde dehydrogenase, HIV nucleocapsid p7 | |||
| IOX1 | King et al. 2010 | KDM3A, KDM4A, KDM4C, KDM4D, KDM4E, KDM6A, KDM6B | KDM2A, KDM5C, PHF8, FIH, PHD2 | ||
| ML324 | Rai et al. 2010 | KDM4E | |||
| NOG | Cloos et al. 2006 | KDM2A, KDM4A, KDM4C, KDM4D, KDM5C, KDM6A, KDM6B, PHD2 | KDM4E, PHF8, FIH | Hopkinson et al. 2013 | |
Inhibitors in bold have shown cytotoxic effects, and those marked with an asterisk have shown efficacy in animal models. In cases in which a single report described multiple, related compounds, only the most potent and/or selective one is listed. Specificity is reported based on the original authors’ interpretation of their data; additional information can be found in the cited references.