1. Epigenetics
  2. Histone Methyltransferase
  3. MS049

MS049 

Cat. No.: HY-100360 Purity: >98.0%
Handling Instructions

MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and do not affect the growth of HEK293 cells.

For research use only. We do not sell to patients.

MS049 Chemical Structure

MS049 Chemical Structure

CAS No. : 1502816-23-0

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10 mM * 1 mL in DMSO USD 66 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and do not affect the growth of HEK293 cells[1].

IC50 & Target

IC50: 34 nM (PRMT4), 43 nM (PRMT6)[1]

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)[1].
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[1].
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[1].

Western Blot Analysis[1]

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[1]

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.
Molecular Weight

248.36

Formula

C₁₅H₂₄N₂O

CAS No.

1502816-23-0

SMILES

CNCCN1CCC(OCC2=CC=CC=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (124.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0264 mL 20.1321 mL 40.2641 mL
5 mM 0.8053 mL 4.0264 mL 8.0528 mL
10 mM 0.4026 mL 2.0132 mL 4.0264 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MS049MS 049MS-049Histone MethyltransferaseepigeneticmodifiersselectiveargininedimethylationtoxicH4R3me2aHEK293cellsInhibitorinhibitorinhibit

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MS049
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