AMI-1 is a cell-permeable inhibitor which inhibits protein arginine N-methyltransferase (PRMT) activity with IC50 of 8.81 µM for PRMT1 and IC50 of 3.04 µM for Hmt1p in vitro. MI-1 does not compete for the AdoMet (S-adenosyl-L-methionine; SAM) binding site and exhibits minimal effects on both SET (Sub39H1, Suv39H2, SET7) and non-SET (DOT1) lysine N-methyltransferases. Furthermore, AMI-1 prevents in vivo arginine methylation of cellular proteins and can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements, thus operating as a brake on certain hormone actions.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cancer | HMTase
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