Cell-permeable, potent, highly selective, reversible and SAM-competitive DOT1L inhibitor
Massonianoside B is a cell-permeable, potent, highly selective, reversible and SAM-competitive DOT1L (disruptor of 4 telomeric silencing 1-like) inhibitor that decreases cellular levels of H3K79 methylation and inhibits the MLL fusion target genes HOXA9 and MEIS1 expression. Massonianoside B exhibits anti-leukemic activity. It is metabolically stable in both human and mouse liver microsomes.
Protein methyltransferases (PMTs) are involved in numerous biological processes and have been studied as a promising target class in the field of oncology and other diseases. Disruptor of telomeric silencing 1-like (DOT1L), a histone H3 lysine 79 (H3K79) methyltransferase, plays
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