2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. MS4322

MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).

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

MS4322 Chemical Structure

MS4322 Chemical Structure

CAS No. : 2375432-47-4

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MS4322:

MS4322 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MS4322

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 ))[1].
IC50 & Target

VHL

 

Cereblon

 

MDM2

 

SMYD2

 

SMYD3

 

EHMT1/GLP/KMT1D

 

SETD7/KMT7

 

PRMT4

 

PRMT8

 

EZH1

 

SETDB1/KMT2G

 

SETD8/KMT5A

 

PRMT5

 

EZH2

 

SUV39H2/KMT1B

 

SETD2/KMT3A

 

PRMT1

 

PRMT6

 

DOT1L

 

EHMT2/G9a/KMT1C

 

NSD2

 

PRMT3

 

PRMT7

 

In Vitro

MS4322 (0.05-5 μM, 6 days) effectively reduces the PRMT5 protein level in a concentration dependent manner, with a Dmax of 74 % in MCF-7 cells[1].
MS4322 (5 μM, 7 days) degrades the PRMT5 protein through a PRMT5-, VHL-, and proteasome-dependent mechanism in MCF-7 cells[1].
MS4322 (0.1-10 μM, 6 days) exhibits antiproliferative effect mainly because of its PRMT5 degradation activity but not its PRMT5 inhibitory activity in MCF-7 cells[1].
MS4322 (5 μM, 6 days) also effectively reduces the PRMT5 protein level and inhibits growth in multiple cancer cell lines (HeLa, A549, A172, and Jurkat cells)[1].

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

MS4322 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MCF-7, HeLa, A549, A172, Jurkat cells
Concentration: 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 6 days
Result: Potently inhibited MCF-7 cell proliferation in a concentration-dependent manner.
Inhibited HeLa, A549, A172, Jurkat cells proliferation.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.05-5 μM(6 days); 5 μM (0-8 days); 0-3 μM(6 days); 5 μM (7 days); 5 μM (6 days)
Incubation Time: 6 days; 0-8 days; 7 days;
Result: Reduced the PRMT5 protein level (0.05-5 μM, 6 days).
Reduced the PRMT5 protein level in a time-dependent manner (5 μM, 0-8 days).
Inhibited SDMA(0-3 μM,6 days).
Reduced the PRMT5 protein level in MCF-7 cells in a PRMT5-, E3 ligase VHL-, and proteasome-dependent manner (5 μM, 7 days).
PRMT5 degradation was reversible (5 μM, 6 days).

Western Blot Analysis[1]

Cell Line: HeLa, A549, A172, Jurkat cells
Concentration: 5 μM
Incubation Time: 6 days
Result: Significantly reduced PRMT5 protein levels in Hela (cervical cancer), A549 (lung adenocarcinoma), A172 (GBM), and Jurkat (leukemia) cells.
In Vivo

MS4322 (150 mg/kg, i.p., single dose, male Swiss albino mice) results in good exposure levels in plasma and reaches the highest plasma concentration (14 μM) 2 hours after administration. After 12 hours, the concentration of MS4322 is still above 100 nM. In addition, MS4322 is well tolerated in treated mice. [1].

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

1101.32

Formula

C55H76N10O12S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=NC=NC(NC2CN(C(COCCOCCOCCOCCOCC(N[C@H](C(N3[C@H](C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)C[C@@H](O)C3)=O)C(C)(C)C)=O)=O)C2)=C1)NC[C@H](O)CN6CC7=C(C=CC=C7)CC6
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 : 100 mg/mL (90.80 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 0.9080 mL 4.5400 mL 9.0800 mL
5 mM 0.1816 mL 0.9080 mL 1.8160 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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 (2.27 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 (2.27 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9080 mL 4.5400 mL 9.0800 mL 22.7000 mL
5 mM 0.1816 mL 0.9080 mL 1.8160 mL 4.5400 mL
10 mM 0.0908 mL 0.4540 mL 0.9080 mL 2.2700 mL
15 mM 0.0605 mL 0.3027 mL 0.6053 mL 1.5133 mL
20 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1350 mL
25 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9080 mL
30 mM 0.0303 mL 0.1513 mL 0.3027 mL 0.7567 mL
40 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5675 mL
50 mM 0.0182 mL 0.0908 mL 0.1816 mL 0.4540 mL
60 mM 0.0151 mL 0.0757 mL 0.1513 mL 0.3783 mL
80 mM 0.0114 mL 0.0568 mL 0.1135 mL 0.2838 mL
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MS4322 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:

MS43222375432-47-4YS43-22MS 4322MS-4322PROTACsHistone MethyltransferasecancerantiproliferativeMCF-7HeLaA549A172Jurkat cellsInhibitorinhibitorinhibit

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