|Solubility:||DMSO up to 100 mM|
|Chemical Name:||2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinic acid|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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-binding site. 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
- 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.
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