MS049

SKU: orb1302906

Description

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 (CARM1) and PRMT6, exhibiting IC50 values of 34 nM and 43 nM, respectively. This compound is a valuable chemical probe for investigating the roles of these methyltransferases in cancer, inflammation, and other epigenetic-regulated processes in both cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1502816-23-0
• MW: 248.36
• Purity: 98.91% (May vary between batches)
• Formula: C₁₅H₂₄N₂O
• SMILES: CNCCN1CCC(CC1)OCc1ccccc1
• Target: Histone Methyltransferase
• Solubility: DMSO:55 mg/mL (221.45 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.05 mM)

Bioactivity

• Target IC50:
  PRMT6:43 nM|PRMT4:34 nM|PRMT8:1600 nM
• In Vitro:
  In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells. 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.
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• Cell Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PRMT6, PRMT4, selective, toxic, cells, dimethylation, arginine, modifiers, MS049, MS-049, MS 049, inhibit, H4R3me2a, epigenetic, Histone Methyltransferase, HistoneMethyltransferase, Inhibitor, HEK293

Compound Identifiers

PubChem CID

53868701