MS049

Catalog No.S8147 Batch:S814701

Technical Data

Formula	C₁₅H₂₆Cl₂N₂O
Molecular Weight	321.29	CAS No.	2095432-59-8
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)
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

References

[1] Shen Y, et al. J Med Chem. 2016, 59(19):9124-9139.

Selleck's MS049 has been cited by 2 publications

Hypoxia stimulates SUMOylation-dependent stabilization of KDM5B [ Research Square, 2021, 10.21203/rs.3.rs-620216/v1]	PubMed: None
Arginine Methylation-Dependent LSD1 Stability Promotes Invasion and Metastasis of Breast Cancer [ EMBO Rep, 2020, 21(2):e48597]	PubMed: 31833203

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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