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EPZ004777 is a potent and selective inhibitor of DOT1L, a protein methyltransferase catalyzing the methylation of lysine 4 of histone H3 (H3K4), with the half maximal inhibition concentration IC50 value of 400 pM [1].

EPZ004777 has been found to concentration-dependently inhibit the H3K79 methylation in a variety of mixed lineage leukemia (MLL) cells, including MLL-rearranged acute myeloid leukemia (MOLM-13 and MLL-AF9), MLL-rearranged biphenotypic leukemia (MV4-11 and MLL-AF4) and non-MLL-rearranged T cell acute leukemia cells [1].

Additionally, EPZ004777 exhibits anti-proliferative activity against both MLL-rearranged and non-rearranged human leukemia cell lines, including RS4;11 (IC50: 6.47 μM), SEM (IC50: 1.72 μM), MV4-11 (IC50: 0.17 μM), THP-1 (IC50: 3.36 μM), MOLM-13 (IC50: 0.72 μM), KOPN-8 (IC50: 0.62 μM), REH (IC50: 13.9 μM), Kasumi-1 (IC50: 32.99 μM) and 697 (IC50: 36.57 μM) [1].

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