MS049 2HCl (1502816-23-0(free base))

SKU: orb1689994

Description

MS049 is a potent and selective small molecule inhibitor of PRMT4 (CARM1) and PRMT6, with IC50 values of 34 nM and 43 nM, respectively. It shows high selectivity over other PRMTs and methyltransferases. This inhibitor is a valuable chemical probe for investigating the roles of these enzymes in cancer, inflammation, and other diseases in both cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• MW: 321.28
• Purity: 99.90% (May vary between batches)
• Formula: C₁₅H₂₆Cl₂N₂O
• SMILES: Cl.Cl.CNCCN1CCC(CC1)OCc2ccccc2
• Target: Histone Methyltransferase
• Solubility: DMSO:30 mg/mL (93.38 mM);PBS(pH7.2):10 mg/mL (31.13 mM);Ethanol:30 mg/mL (93.38 mM)

Bioactivity

• Target IC50:
  PRMT4:34 nM|PRMT6:43 nM
• In Vitro:
  MS049 has been shown to reduce the H3R2me2a mark in HEK293 cells with an IC50 value of 0.97 μM and also, unexpectedly, to reduce H4R3me2a in HEK293 cells.
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• Cell Research:
  HEK293 cells were grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 units/mL) and streptomycin (100 μg/mL). 30% confluent cells were treated with different concentrations of compounds in triplicates or DMSO control for 72 h. Cells were lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% TritonX-100, 12.5 U/mL benzonase, complete EDTA-free protease inhibitor cocktail ). After 3 min incubation at RT, SDS was added to final 1% concentration. Lysates were run on SDS-PAGE and immunoblotting was done as outlined below to determine Med12-Rme2a levels in Western blot. They are for reference only.
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Storage & Handling

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

Alternative Names

Histone Methyltransferase, HistoneMethyltransferase, MS049 2HCl (1502816230(free base)), MS-049 2HCl (1502816-23-0(free base)), MS049 2HCl (1502816-23-0(free base)), MS049 2HCl (1502816 23 0(free base)), PRMT4, PRMT6

Compound Identifiers

PubChem CID

129626588