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AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It exerts its inhibitory effects on PRMTs by blocking peptide-substrate binding.
Potent, cell-permeable, and reversible inhibitor of PRMTs.
Inhibits type I PRMTs and type II PRMT5.
Specifically inhibits arginine methyltransferase activity, not lysine, and does not compete for the AdoMet binding site.
Inhibits methylation of GFP-Npl3 and cellular proteins.
Inhibits the cell viability of sarcoma in S180 and U2OS cells in a time- and dose-dependent manner in vitro.
Reduces S180 cell viability through the induction of cell apoptosis.
Inhibits S180 viability in vivo.
Downregulates PRMT5 and decreases levels of H4R3me2s and H3R8me2s in a tumor xenograft model.
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