Product Size
25 mg
125 mg
Custom Size
Product Overview
Description
Potent, selective, cell-active PRMT inhibitor.
Biological Description
MS023 is a potent, selective, and cell-active Type I PRMT inhibitor. IC50 values are 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6) and 5 nM (PRMT8). It potently reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 values of 9 nM and 56 nM, respectively. MS023 also inhibits cell growth and potentially induces growth arrest and flattening morphology at low concentrations. It displayed high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but displayed no activity against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. Cellular levels of histone arginine asymmetric dimethylation were potently reduced by MS023. It also reduced global levels of arginine asymmetric dimethylation whilst increasing levels of arginine monomethylation and symmetric dimethylation in cells. MS023 is active in cells.
Solubility Overview
Soluble in DMSO to 100 mM and in ethanol to 100 mM.
Chemical Properties
Chemical Name
N1-Methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine
Molecular Weight (Da)
287.40
Molecular Formula
C17H25N3O
SMILES
CC(C)OC1=CC=C(C=C1)C2=CNC=C2CN(C)CCN
Storage & Handling
Storage Instructions
Shipped at 4 °C. Store at -20 °C.
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20 °C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
