Art. -Nr.: HY-133129

MS1943

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

MS1943 is an orally active selective HyT degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC₅₀=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)).

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Reinheit: 98.92%
CAS. Nr.: 2225938-17-8
Formel: C₄₂H₅₄N₈O₃
Molecular Weight:718.93

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MS1943 Chemical Structure

CAS. Nr.: 2225938-17-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EZH2 methyltransferase

120 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC₅₀	>40 μM Compound: MS1943	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-468	IC₅₀	3.41 μM Compound: MS1943	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]

In Vitro

MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI₅₀ of 2.2 μM^[1].
MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells^[1].
MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed^[1].

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

Cell Viability Assay^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

0.625, 1.25, 2.5, 5 μM
Incubation Time:

3 days
Result:

Inhibits cell growth with an GI₅₀ of 2.2 µM.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

1.25, 2.5, 5.0 μM
Incubation Time:

2 days
Result:

Reduced EZH2 protein levels in a concentration- and time-dependent manner.

In Vivo

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth^[1].
MS1943 induces apoptosis in the MDA-MB-468 xenograft model^[1].
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 μM and resulted in plasma concentrations above its cellular IC₅₀ value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 μM, but plasma concentrations were below the cellular IC₅₀ value^[1].

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

Animal Model:

Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)^[1]
Dosage:

150 mg/kg body weight
Administration:

i.p.; once daily for 36 days
Result:

Suppresses tumor growth.

Chemical Information

CAS. Nr. 2225938-17-8
Appearance Solid
Molecular Weight 718.93
Formel C₄₂H₅₄N₈O₃
Color Light yellow to yellow
SMILES

CC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[C@H]8C[C@H](C[C@H](C8)C7)C6)=O)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Biochem Pharmacol

Momordin Ic suppresses breast cancer growth by targeting ACTL8‑dependent glutamine metabolism and PI3K/AKT/mTOR-MYC. [Abstract]

2026 May:247:117761. PMID: 41621692

MS1943 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2026 May:247:117761. [Abstract]

Western blot analysis showing ACTL8 protein levels in BC cells treated with DMSO, Momordin Ic, Thiostrepton, XY028-140, MS1943, or dBET1(10 μM each) for 24 h, indicating that Momordin Ic markedly reduced ACTL8 expression.
bioRxiv

Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]

2025 Sep 18:2025.09.16.676613. PMID: 41000734
bioRxiv

2025 Jul 18.
Research Square Preprint

2021 Dec.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (173.87 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

1.3910 mL

6.9548 mL

13.9096 mL

5 mM

0.2782 mL

1.3910 mL

2.7819 mL

10 mM

0.1391 mL

0.6955 mL

1.3910 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, 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.

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: ≥ 6.25 mg/mL (8.69 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (8.69 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (8.69 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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 (275 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Ma A, et al. Discovery of a first-in-class EZH2 selective degrader[J]. Nature chemical biology, 2020, 16(2): 214-222. [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, 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	1.3910 mL	6.9548 mL	13.9096 mL	34.7739 mL
	5 mM	0.2782 mL	1.3910 mL	2.7819 mL	6.9548 mL
	10 mM	0.1391 mL	0.6955 mL	1.3910 mL	3.4774 mL
	15 mM	0.0927 mL	0.4637 mL	0.9273 mL	2.3183 mL
	20 mM	0.0695 mL	0.3477 mL	0.6955 mL	1.7387 mL
	25 mM	0.0556 mL	0.2782 mL	0.5564 mL	1.3910 mL
	30 mM	0.0464 mL	0.2318 mL	0.4637 mL	1.1591 mL
	40 mM	0.0348 mL	0.1739 mL	0.3477 mL	0.8693 mL
	50 mM	0.0278 mL	0.1391 mL	0.2782 mL	0.6955 mL
	60 mM	0.0232 mL	0.1159 mL	0.2318 mL	0.5796 mL
	80 mM	0.0174 mL	0.0869 mL	0.1739 mL	0.4347 mL
	100 mM	0.0139 mL	0.0695 mL	0.1391 mL	0.3477 mL

MS1943

4 Cited Publications

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MS1943

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MS1943

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS1943

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MS1943

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS1943 Related Classifications

HY-133129 Related Classifications