Abstract
Replying to B. Heinemann et al. Nature 514, 10.1038/nature13688 (2014)
We welcome the accompanying Comment1 by Heinemann et al., in which the authors use an extensive panel of sensitive KDM assays to independently confirm our results2 that GSK-J1 is a potent KDM6 inhibitor. Additionally, Heinemann et al.1 demonstrate that GSK-J1 has some, albeit weaker, activity towards KDM5B and KDM5C, for which we only had preliminary data available at the time of our original publication. As our jumonji assay portfolio expands, we have continued to update the GSK-J1 activity profile on the SGC website (http://www.thesgc.org/chemical-probes/GSKJ1); this includes KDM5 inhibition activity by GSK-J1 similar to that reported by Heinemann. In conclusion, GSK-J1 remains the most selective KDM inhibitor yet disclosed and thus a valuable chemical tool.
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References
Heinemann, B. et al. Inhibition of demethylases by GSK-J1/J4. Nature 514, http://dx.doi.org/10.1038/nature13688 (2014)
Kruidenier, L. et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488, 404–408 (2012)
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Kruidenier, L., Chung, Cw., Cheng, Z. et al. Kruidenier et al. reply. Nature 514, E2 (2014). https://doi.org/10.1038/nature13689
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DOI: https://doi.org/10.1038/nature13689
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