2. Epigenetics
  3. Histone Methyltransferase
  4. MS049

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 does not affect the growth of HEK293 cells.

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MS049 Chemical Structure

MS049 Chemical Structure

CAS No. : 1502816-23-0

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MS049:

MS049 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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 does not affect the growth of HEK293 cells[1].

IC50 & Target[1]

PRMT4

34 nM ()

PRMT6

43 nM ()

PRMT8

1600 nM ()

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.97 μM
Compound: 17; MS049
Inhibition of wild-type FLAG-tagged PRMT6 (unknown origin) expressed in HEK293 cells assessed as reduction in H3R2me2a level measured after 20 hrs by western blot analysis
Inhibition of wild-type FLAG-tagged PRMT6 (unknown origin) expressed in HEK293 cells assessed as reduction in H3R2me2a level measured after 20 hrs by western blot analysis
[PMID: 27584694]
HEK293 IC50
1.4 μM
Compound: 17; MS049
Inhibition of PRMT4 in HEK293 cells assessed as reduction in Med12-Rme2a level measured after 72 hrs by western blot analysis
Inhibition of PRMT4 in HEK293 cells assessed as reduction in Med12-Rme2a level measured after 72 hrs by western blot analysis
[PMID: 27584694]
MT4 IC50
34 nM
Compound: 17; MS049
Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H3 (1 to 25) peptide as substrate and [3H]-SAM measur
Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H3 (1 to 25) peptide as substrate and [3H]-SAM measur
[PMID: 27584694]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS049 Related Antibodies

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.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (402.64 mM)

DMSO : ≥ 31 mg/mL (124.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (402.64 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

SDS (479 KB)

COA (243 KB) HNMR (245 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 4.0264 mL 20.1321 mL 40.2641 mL 100.6603 mL
5 mM 0.8053 mL 4.0264 mL 8.0528 mL 20.1321 mL
10 mM 0.4026 mL 2.0132 mL 4.0264 mL 10.0660 mL
15 mM 0.2684 mL 1.3421 mL 2.6843 mL 6.7107 mL
20 mM 0.2013 mL 1.0066 mL 2.0132 mL 5.0330 mL
25 mM 0.1611 mL 0.8053 mL 1.6106 mL 4.0264 mL
30 mM 0.1342 mL 0.6711 mL 1.3421 mL 3.3553 mL
40 mM 0.1007 mL 0.5033 mL 1.0066 mL 2.5165 mL
50 mM 0.0805 mL 0.4026 mL 0.8053 mL 2.0132 mL
60 mM 0.0671 mL 0.3355 mL 0.6711 mL 1.6777 mL
80 mM 0.0503 mL 0.2517 mL 0.5033 mL 1.2583 mL
100 mM 0.0403 mL 0.2013 mL 0.4026 mL 1.0066 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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MS049 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS0491502816-23-0MS 049MS-049Histone MethyltransferaseepigeneticmodifiersselectiveargininedimethylationtoxicH4R3me2aHEK293cellsInhibitorinhibitorinhibit

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