MS-049

SKU: orb1226176

Description

A potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50 of 34±10 nM and 43±7 nM, respectively; displays >30-fold and >300-fold selectivity over PRMT8 and PRMT1/3, does not inhibits PKMTs, DNMTases, RNA methyltransferases; reduces the H3R2me2a mark in HEK293 cells with IC50 of 0.97 uM.

Key Properties

• CAS Number: 1502816-23-0
• MW: 248.3639
• Purity: >98% (HPLC)
• Formula: C₁₅H₂₄N₂O
• SMILES: CNCCN1CCC(OCC2=CC=CC=C2)CC1
• Target: HMTase
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vitro:
  MS049 (0.1-10 μM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50 = 0.97±0.05 μM). MS049 (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50 = 1.4±0.1 μM) in HEK293 cells. MS049 is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets. Western blot analysis. Cell line: HEK293 cells. Concentration: 0.1, 1, 10 μM Incubation time: 20 hours. Result: Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC50 = 0.97±0.05 μM). Western blot analysis. Cell line: HEK293 cells. Concentration: 0.1, 1, 10, 100 μM Incubation time: 72 hours. Result: Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50 = 1.4±0.1 μM) in HEK293 cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MS049

Quick Database Links

Gene Symbol

HMTase