Protein Arginine N-Methyltransferase Inhibitor; AMI-1

Biochem/physiol Actions

Primary TargetProtein arginine N-methyltransferases (PRMTs)

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 8.81 µM for PRMT1 and 3.03 for yeast-RMT1p

Cell permeable: yes

General description

A cell-permeable, symmetrical sulfonated urea compound that acts as a potent, specific and non-AdoMet (S-adenosyl-L-methionine, SAM)-competitive inhibitor of protein arginine N-methyltransferases (PRMTs; IC₅₀ = 8.81 µM for PRMT1 and 3.03 for yeast-RMT1p) with minimal effect on lysine methyltransferases. Inhibits nuclear receptor reporter gene activation in MCF-7 cells, and HIV-1 RT polymerase (IC₅₀ = 5 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Cheng, D., et al. 2004. J. Biol. Chem.279, 23892.Skillman, A.G., et al. 2002. Bioorg. Chem.30, 443.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)