2. Epigenetics
  3. Histone Methyltransferase
  4. MS117

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.

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

MS117 Chemical Structure

MS117 Chemical Structure

CAS No. : 2702280-86-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 580 In-stock
25 mg USD 1100 In-stock
50 mg USD 1700 In-stock
100 mg USD 2500 In-stock
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

MS117 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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM[1].

IC50 & Target

PRMT6

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
1.3 μM
Compound: 4; MS117
Inhibition of Flag-tagged PRMT6 (unknown origin) expressed in HEK293 cells incubated for 20 hrs assessed as reduction in H3R2me2a levels
Inhibition of Flag-tagged PRMT6 (unknown origin) expressed in HEK293 cells incubated for 20 hrs assessed as reduction in H3R2me2a levels
[PMID: 32367723]
MCF7 IC50
5.6 μM
Compound: 4; MS117
Inhibition of PRMT1 in human MCF7 cells assessed as reduction in H4R3me2a levels incubated for 2 days by fluorescence based assay
Inhibition of PRMT1 in human MCF7 cells assessed as reduction in H4R3me2a levels incubated for 2 days by fluorescence based assay
[PMID: 32367723]
In Vitro

MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner[1].
MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC50 = 0.1 ± 0.025 μM) and PRMT8 (IC50 = 0.11 ± 0.01 μM) [1].

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

MS117 Related Antibodies
Molecular Weight

298.38

Formula

C17H22N4O
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

NCCN(C)CC1=CNC=C1C2=CC=CC(NC(C=C)=O)=C2
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: 

DMSO : 100 mg/mL (335.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3514 mL 16.7572 mL 33.5143 mL
5 mM 0.6703 mL 3.3514 mL 6.7029 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (8.38 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 (8.38 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 1 mM 3.3514 mL 16.7572 mL 33.5143 mL 83.7858 mL
5 mM 0.6703 mL 3.3514 mL 6.7029 mL 16.7572 mL
10 mM 0.3351 mL 1.6757 mL 3.3514 mL 8.3786 mL
15 mM 0.2234 mL 1.1171 mL 2.2343 mL 5.5857 mL
20 mM 0.1676 mL 0.8379 mL 1.6757 mL 4.1893 mL
25 mM 0.1341 mL 0.6703 mL 1.3406 mL 3.3514 mL
30 mM 0.1117 mL 0.5586 mL 1.1171 mL 2.7929 mL
40 mM 0.0838 mL 0.4189 mL 0.8379 mL 2.0946 mL
50 mM 0.0670 mL 0.3351 mL 0.6703 mL 1.6757 mL
60 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3964 mL
80 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
100 mM 0.0335 mL 0.1676 mL 0.3351 mL 0.8379 mL
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MS117 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:

MS1172702280-86-0MS 117MS-117Histone MethyltransferaseInhibitorinhibitorinhibit

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