HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM, HDAC1: IC50=134 nM, HDAC2: IC50=284 nM, HDAC3: IC50=173 nM, HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 µM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.
Target-Kategorie:
HDAC|||Autophagy|||Apoptosis|||Xanthine Oxidase
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