MS023
Noncompetitive inhibitor of PRMT1, PRMT6, CARM1, PRMT8, PRMT3
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
(last updated: 31 May 2016 )
SERP Ratings
(last updated: 7 Jun 2016 )
SERP Ratings
SERP Comments:
MS023 is a potent and non-selective inhibitor of Type-1 PRMT's and is structurally related to the PRMT6 inhibitor EPZ020411. MS023 binding to PRMT6 has been confirmed using orthogonal assays, including DSF (at high concentrations) and ITC. MS023 does not inhibit a panel of 25 PKMTs (protein lysine methyltransferases), and DNMTs (DNA methyltransferases) and three histone lysine demethylases (IC50<100nM). Inhibition of PRMT1 and PRMT6 with M023 translates to inhibition of asymmetric dimethylation of H4R3 (in MCF7 cells) and H3R2 (in HEK293 cells)(IC50<100nM). Pan-inhibition of Type 1 PRMT's with M023 translates to inhibition of global mono- and asymmetric dimethylation of arginine residues in MCF7 and HEK293 cells. MS023 did not have a major influence in cell viability (8 cell lines) after 96h, at concentrations up to 10µM, except for HEK293 cells. No ADME of physicochemical information on MS023 is available. MS023 (and its inactive analogue MS094) should be used in-cell based assays to interrogate the pharmacological consequences of non-selective PRMT inhibition.
(last updated: 7 Jun 2016 )
Portal Comments
In a 2023 study, Hu et al. evaluated MS023 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations equal or exceeding 1 uM. (DOI: 10.1016/j.chembiol.2023.09.003)
(last updated: 7 Nov 2023)