2. PROTAC Epigenetics Apoptosis
  3. HyT Histone Methyltransferase Apoptosis
  4. MS1943

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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CAS 番号 : 2225938-17-8

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 158 在庫あり
Solution
10 mM * 1 mL in DMSO USD 158 在庫あり
Solid
5 mg $100 在庫あり
10 mg $170 在庫あり
25 mg $336 在庫あり
50 mg $590 在庫あり
100 mg $1098 在庫あり
250 mg $2200 在庫あり
500 mg $3300 在庫あり
1 g $4950 在庫あり
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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

MS1943 関連抗体

Top Publications Citing Use of Products

    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.

    Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    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

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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))[1].

    IC50 & Target[1]

    EZH2 methyltransferase

    120 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    MDA-MB-231 IC50
    > 40 3
    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 3
    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]
    体外実験

    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.

    MS1943 関連抗体

    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.
    体内実験

    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.
    分子量

    718.93

    分子式

    C42H54N8O3
    CAS 番号
    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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.
    In Vivo Dissolution Calculator
    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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    % 
    +
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    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.
    純度とドキュメンテーション

    純度: 98.92%

    COA (246 KB) LCMS (95 KB)

    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
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    MS1943 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    MS19432225938-17-8MS 1943MS-1943HyTHistone MethyltransferaseApoptosisHydrophobie taggingtriple-negativebreastcancerTNBCproliferationfirst-in-classcytotoxicdegradermethyltransferaseapoptosisInhibitorinhibitorinhibit

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    製品名:
    MS1943
    製品番号:
    HY-133129
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