MS023 potently inhibits PRMT1 (IC50 = 30 ± 9 nM), PRMT3 (IC50 = 119 ± 14 nM), PRMT4 (IC50 = 83 ± 10 nM), PRMT6 (IC50 = 4 ± 0.5 nM), and PRMT8 (IC50 = 5 ± 0.1 nM). MS023 displays high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreases cellular levels of histone arginine asymmetric dimethylation. It also reduces global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells.
|Cell lines||MCF7, U2Os, HFF, HCT116, HEK293 , A549, MDA-MB-231 and T98G|
|Preparation method||Different cell lines are seeded on 96-well plates at density 3000/well and treated with MS023 at 0, 0.1, 1, 10, 50 and 100 μM concentrations for 96 h. MCF7, U2Os, HFF, HCT116, HEK293 are grown in DMEM and A549, MDA-MB-231 and T98G in RPMI supplemented with 10% FBS, penicillin (100 U/mL) and streptomycin (100 mg/mL). The inhibitor is replaced after 48 h. The confluency is measured using IncuCyte™ ZOOM live cell imaging device and analysed with IncuCyte™ ZOOM (2015A) software based on phase contrast images.|
|Incubation time||96 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
Eram MS, et al. ACS Chem Biol. 2016 Mar 18;11(3):772-781. PMID: 26598975.
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