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IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively[1][2]. IOX1 also inhibits ALKBH5[3].

IOX1 (0-200 μM; 2 hours) inhibits the proliferation and migration of vascular smooth muscle cells (VSMCs) stimulated with angiotensin II (Ang II) in a concentration-dependent manner[2].IOX1 (200 μM; 24 hours) blocks the cell cycle progression of angiotensin II (Ang II)-VSMCs by increasing the percentage of cells in the G0/G1 phase[2].IOX1 (50-200 μM; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent[2].IOX1 (50-200 μM; 2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3[2].

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