Description
A pan-inhibitor of 2-OG-dependent demethylases and oxygenases; inhibits JMJD2C, JMJD2E, JMJD1A, JMJD2A, JARID1C, and JMJD3 in cell-free assays (IC50s = 0.6, 2.3, 1.8, 0.1, 19, and 1.4 µM, respectively); inhibits demethylation of H3K9Me3 by JMJD2A in HeLa cells (IC50 = 86.5 µM); inhibits HIF-PH2 and FIH (IC50s = 14.3 and 20.5 µM, respectively); reduces angiotensin II-induced proliferation and migration of primary rat VSMCs at 200 µM); active against E. coli and A. baumannii in vitro; increases survival, decreases lung PMN infiltration, and reduces serum and lung TNF-α, IL-1β, and IL-6 levels in a mouse model of LPS-induced endotoxemia at 20 mg/kg; decreases tumor weight and volume and increases intratumoral T cell infiltration in a CT26 murine model of colon cancer when administered alone or in combination with bevacizumab