MS1943
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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.92%
- CAS 番号: 2225938-17-8
- 分子式: C42H54N8O3
- 分子量:718.93
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 MS1943
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Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
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EZH2 methyltransferase 120 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | IC50 |
>40 μM
Compound: MS1943
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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
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[PMID: 35623249] |
| MDA-MB-468 | IC50 |
3.41 μM
Compound: MS1943
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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
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[PMID: 35623249] |
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.
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Cell Line:MDA-MB-468 cells
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Concentration:0.625, 1.25, 2.5, 5 μM
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Incubation Time:3 days
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Result:Inhibits cell growth with an GI50 of 2.2 µM.
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Cell Line:MDA-MB-468 cells
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Concentration:1.25, 2.5, 5.0 μM
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Incubation Time:2 days
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Result:Reduced EZH2 protein levels in a concentration- and time-dependent manner.
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.
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Animal Model:Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)[1]
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Dosage:150 mg/kg body weight
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Administration:i.p.; once daily for 36 days
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Result:Suppresses tumor growth.
化学情報
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CAS 番号 2225938-17-8
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性状 Solid
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分子量 718.93
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分子式 C42H54N8O3
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Color Light yellow to yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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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.
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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 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (396 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 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 関連分類
HY-133129 関連分類
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