iPHF8 is a specific inhibitor (IC50 = 2.01 µM, EC50 = 2 µM in HeLa cells) of the human non-heme 2-oxoglutarate JmjC domain oxygenase/lysine demethylase PHF8. PHF8 also demethylates the transcription factor YY1 acting as a co-repressor for many electron transport chain genes driving mROS production and cancer development. It inhibited mROS production, cell proliferation, and colony formation in HCT116 and H1299 cells. iPHF8 significantly decreased tumor size in HCT116 derived tumors and colon cancer patient-derived xenografts.
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