Art. -Nr.: HY-141877

MS4322

(Synonyms: YS43-22)

1 Cited Publications

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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 )).

(Pink: Histone Methyltransferase ligand (HY-173092); Blue: VHL ligand (HY-112078); Black: linker (HY-124780)).

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Reinheit: 99.14%
CAS. Nr.: 2375432-47-4
Formel: C₅₅H₇₆N₁₀O₁₂S
Molecular Weight:1101.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS4322 Chemical Structure

CAS. Nr.: 2375432-47-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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].
(Pink: Histone Methyltransferase ligand (HY-173092); Blue: VHL ligand (HY-112078); Black: linker (HY-124780)).

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

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

MS4322 (0.05-5 μM, 6 days) effectively reduces the PRMT5 protein level in a concentration dependent manner, with a D_max 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.

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.

Chemical Information

CAS. Nr. 2375432-47-4
Appearance Solid
Molecular Weight 1101.32
Formel C₅₅H₇₆N₁₀O₁₂S
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
Synonyms

YS43-22
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Cancer Res Commun

PRMT5 Inhibitors Regulate DNA Damage Repair Pathways in Cancer Cells and Improve Response to PARP Inhibition and Chemotherapies. [Abstract]

2023 Nov 6;3(11):2233-2243. PMID: 37861290

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9080 mL

4.5400 mL

9.0800 mL

5 mM

0.1816 mL

0.9080 mL

1.8160 mL

10 mM

0.0908 mL

0.4540 mL

0.9080 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Shen Y, et al. Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders. J Med Chem. 2020 Sep 10;63(17):9977-9989. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MS4322

1 Cited Publications

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MS4322

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) MS4322

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS4322

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) MS4322

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS4322 Related Classifications

HY-141877 Related Classifications