MS023

Catalog No.S8112

MS023 Chemical Structure

Molecular Weight(MW): 287.40

MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.

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Biological Activity

Description MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
Targets
PRMT6 [1]
(Cell-free assay)
PRMT8 [1]
(Cell-free assay)
PRMT1 [1]
(Cell-free assay)
PRMT4 [1]
(Cell-free assay)
PRMT3 [1]
(Cell-free assay)
4 nM 5 nM 30 nM 83 nM 119 nM
In vitro

MS023 potently reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 of 9 nM and 56 nM, respectively. MS023 also inhibits cell growth and potentially induces growth arrest and flattening morphology at low concentrations. MS023 displayed high potency for type I PRMTs including PRMT1, 3, 4, 6 and 8, but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreased cellular levels of histone arginine asymmetric dimethylation. It also reduced global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells[1].

Protocol

Kinase Assay:

[1]

+ Expand

PRMT Biochemical Assays:

A scintillation proximity assay (SPA) is used for assessing the effect of test compounds on inhibiting the methyl transfer reaction catalyzed by PRMTs. In brief, the tritiated S-adenosyl-L-methionine (3H-SAM) is used as the donor of methyl group. The (3H) methylated biotin labeled peptide is captured in a streptavidin/scintillant-coated microplate, which brings the incorporated 3H-methyl and the scintillant to close proximity resulting in light emission that is quantified by tracing the radioactivity signal (counts per minute) as measured by a TopCount NXT Microplate Scintillation and Luminescence Counter. When necessary, nontritiated SAM is used to supplement the reactions. The IC50 values are determined under balanced conditions at Km concentrations of both substrate and cofactor by titration of test compounds in the reaction mixture.
Cell Research:

[1]

+ Expand
  • Cell lines: MCF7, U2Os, HFF, HCT116, HEK293 , A549, MDA-MB-231 and T98G
  • Concentrations: ~100 mM
  • Incubation Time: --
  • 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 mM 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-1) and streptomycin (100 mg mL-1). 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (198.32 mM)
Ethanol 57 mg/mL (198.32 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 287.40
Formula

C17H25N3O

CAS No. 1831110-54-3
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID