EPZ-6438 is an inhibitor of EZH2, a histone methyltransferase (HMT) responsible for methylation of lysine and arginine residues and controls gene transcription fidelity in cells. EPZ-6438 displays anticancer chemotherapeutic activity in in vivo models by inducing regression of malignant or atypical teratoid rhabdoid tumors containing altered or mutant SWI/SNF ATP-dependent chromatin remodelers.
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