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9(12):2126-39
and the apparent Ki is 2
(2010) Blood
and in engineered cells overexpressing oncogenic RAS
KDM5-C49 - JARID1 Histone Demethylases Inhibitor. CAS# 1596348-16-1 319 9(12):2126-39KDM5 C49, CAS No. 1596348 16 1, 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 M for inhibiting demthylation of H3K4 in
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