Uses
EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research[1].
References
[1] Bon C, et al. Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein. Molecules. 2021 Aug 31;26(17):5300. DOI:
10.3390/molecules26175300[2] Lillico R, et al. Selective DOT1L, LSD1, and HDAC Class I Inhibitors Reduce HOXA9 Expression in MLL-AF9 Rearranged Leukemia Cells, But Dysregulate the Expression of Many Histone-Modifying Enzymes. J Proteome Res. 2018 Aug 3;17(8):2657-2667. DOI:
10.1021/acs.jproteome.8b00118