AMI-1 (sodium salt)

AMI-1 is a cell permeable inhibitor of PRMTs. It inhibits both yeast Type I arginine methyltransferase Hmt1p and human PRMT1 (IC50 = 3.0 and 8.8 μM, respectively).1 AMI-1 also effectively blocks the activity of PRMTs 3, 4, and 6 but not that of either SET (Sub39H1, Suv39H2, SET7) or non-SET (DOT1) lysine methyltransferases.1 The mechanism of inhibition of PRMTs by AMI-1 involves blocking peptide-substrate binding.2 AMI-1 also inhibits HIV-1 reverse transcriptase (IC50 = 5.0 μM).3WARNING This product is not for human or veterinary use.

[1] DONGHANG CHENG. Small molecule regulators of protein arginine methyltransferases.[J]. The Journal of Biological Chemistry, 2004, 279 23: 23892-23899. DOI: 10.1074/jbc.m401853200
[2] YOU FENG. Inhibitory study of protein arginine methyltransferase 1 using a fluorescent approach[J]. Biochemical and biophysical research communications, 2009, 379 2: Pages 567-572. DOI: 10.1016/j.bbrc.2008.12.119
[3] A.GEOFFREY SKILLMAN . A novel mechanism for inhibition of HIV-1 reverse transcriptase[J]. Bioorganic Chemistry, 2002, 30 6: Pages 443-458. DOI: 10.1016/s0045-2068(02)00502-3