MS049

Catalog No.S8147

MS049 Chemical Structure

Molecular Weight(MW): 321.29

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Targets
PRMT4 [1]
(Cell-free assay)
PRMT6 [1]
(Cell-free assay)
34 nM 43 nM
In vitro

MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM. MS049 demonstrated excellent selectivity over a broad range of epigenetic and nonepigenetic targets. In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells[1].

Protocol

Cell Research:

[1]

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  • Cell lines: HEK293 cells
  • Concentrations: 0, 1, 10, and 50 μM
  • Incubation Time: 96 h
  • Method:

    HEK293 cells grown in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL) were seeded on 96-well plates at density 3000/well and treated with compounds at 0, 1, 10, and 50 μM concentrations for 96 h. The confluency was measured using IncuCyte ZOOM live cell imaging device and analyzed with IncuCyte ZOOM software based on phase contrast images.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (174.29 mM)
Water 56 mg/mL (174.29 mM)
Ethanol 50 mg/mL (155.62 mM)

* 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 321.29
Formula

C15H26Cl2N2O

CAS No. 1502816-23-0(free base)
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