MS1943

Name: MS1943
Brand: MedChemExpress
SKU: HY-133129
Rating: 5.0 (4 reviews)

Cat. No.: HY-133129 Purity: 98.92%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 2225938-17-8

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
250 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	해외재고보유	Estimated Time of Arrival: December 31
5 g	견적 받기
10 g	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE MS1943

: 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.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

EZH2 methyltransferase

120 nM (IC₅₀)

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.

분자량

718.93

화학식

C₄₂H₅₄N₈O₃

CAS No.

2225938-17-8

Appearance

Solid

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

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.
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: ≥ 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.
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.
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

mg/kg

Animal weight
(per animal)

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.

순도&문서

Purity: 98.92%

Select Batch:

Data Sheet (275 KB) SDS (396 KB)

COA (246 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 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.

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MS1943

고객리뷰

MS1943 Related Antibodies

4 Publications Citing Use of MCE MS1943

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

MS1943 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

MS1943 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

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SAFETY DATA SHEET (SDS)

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