Selectivity profiling of the dihydropyrazoles 1 and IOX4 against a panel of human 2OG-dependent dioxygenases.

The IC50 values obtained reveal the selectivity of dihydropyrazoles 1 and IOX4 for PHD2 in comparison with IOX2 and NOG. Assays were carried out as previously reported [9,18,19,38]. PHD2: HIF-prolyl hydroxylase-2, JMJD1A (KDM3A): Lysine-specific demethylase 3A, JMJD2A (KDM4A): Lysine-specific demethylase 4A, JMJD2C (KDM4C): Lysine-specific demethylase 4C, JMJD2E (KDM4E): Lysine-specific demethylase 4E, JMJD3 (KDM6B): Lysine-specific demethylase 6B, FBXL11 (KDM2A): Lysine-specific demethylase 2A, JARID1C (KDM5C): Lysine-specific demethylase 5C, BBOX: γ-butyrobetaine hydroxylase, FIH: factor inhibiting HIF, FTO: fat mass and obesity associated protein. Selectivity profiling of the dihydropyrazoles 1 and IOX4 against a panel of human 2OG-dependent dioxygenases.