Purity ~99% (HPLC). A benzothiadiazolyl-cyclohexenylethylurea compound that binds to protein arginine methyltransferase 3 at the dimer interface and selectively inhibits PRMT3 activity in an allosteric manner (IC50 = 1.6uM), while being non-competitive with respect to AdoMet (S-adenosyl-L-methionine; SAM) or peptide substrates (Ki = 2.9 and 4.2 mM, respectively). Exhibits little or no inhibitory activity against PRMT1/4/5/8 or protein lysine methyltransferases, EHMT1, SUV39H2, SETD7, and SETD8, even at concentrations above 100uM. Although cell-permeable, it is metabolically unstable and therefore not recommended for cell cultures or in vivo applications. Primary Target: PRMT3 Primary Target IC50: 1.6u Molar Mass: 302.4 Solubility: DMSO
Size
10mg
Concentration
n/a
Applications
n/a
Other Names
PRMT Inhibitor VI (1-(Benzo[d][1,2,3]thiadiazol-6-yl)-3-(2-cyclohexenylethyl)urea, 1-(1,2,3-Benzothiadiazol-6-yl)-3-[2-(1-cyclohexen-1-yl)ethyl]urea, Protein Arginine Methyltransferase Inhibitor VI)