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Biological Activity:

KDM5-C49 is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It has IC50 ~40 nM, 160 nM and 100 nM for KDM5A, KDM5B and KDM5C respectively. It has >100-fold selectivity over KDM4 and KDM6 etc. KDM5-C49 occupies the aKG-. The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability, so it has IC50 >1 μM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line and in human breast adenocarcinoma MCF7 tumor cell proliferation assay. Therefore KDM5-C70 was developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use.

How to Use:

In vitro: KDM5-C49 was used at 1-10 μM in vitro.
In vivo: n/a


Reference:

• 1. Marc Labelle, et al. Inhibitors of Histone Demethylases. (2014). PCT WO 2014053491
• 2. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. (2016) Nat Chem Biol. 12(7):539-45.?
• 3. Horton JR, et al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. (2016) Cell Chem Biol. 23(7):769-81.?