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KDM2A/7A-IN-1 is an inhibitor of lysine demethylase 2A (KDM2A) and KDM7A (IC50s = 0.16 and 0.19 µM, respectively).1 It is selective for KDM2A and -7A over KDM3A (IC50 = 39 µM), KDM4A, -4C, and -4D (IC50s = 639, 430, and 321 µM, respectively), KDM5B and -C (IC50s = 17 and 16 µM, respectively), KDM6B (IC50 = 20 µM), and KDM7B (IC50 = 34 µM). KDM2A/7A-IN-1 (1 and 10 µM) inhibits KDM2A-mediated demethylation of dimethylated histone H3 lysine 36 (H3K36me2) in HeLa cells.
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