MS049

Catalog No.S8147 Batch:S814701

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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.)

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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.

Selleck's MS049 has been cited by 3 publications

PRMT6-mediated ADMA promotes p62 phase separation to form a negative feedback loop in ferroptosis [ Theranostics, 2024, 14(10):4090-4106] PubMed: 38994016
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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.