1. Epigenetics
  2. Histone Methyltransferase
  3. Pinometostat

Pinometostat  (Synonyms: EPZ-5676)

製品番号: HY-15593 純度: 99.93%
COA 取扱説明書 Technical Support

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

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。

CAS 番号 : 1380288-87-8

容量 価格(税別) 在庫状況 数量
>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 87 在庫あり
Solution
10 mM * 1 mL in DMSO USD 87 在庫あり
Solid
5 mg $70 在庫あり
10 mg $100 在庫あり
25 mg $210 在庫あり
50 mg $360 在庫あり
100 mg $600 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 28 publication(s) in Google Scholar

Other Forms of Pinometostat:

Top Publications Citing Use of Products

    Pinometostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 10;16(1):2384.  [Abstract]

    Count of Annexin V negative Tet2KO or Tet2WT HPCHOXB4 cells treated with Pinometostat (1μM; 0-20 days) over time normalized to the corresponding untreated sample.

    Pinometostat purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9.  [Abstract]

    Number of hCiPSC colonies induced from hADSCs (hADSCs-0618) with stage II condition (SII, 12 days treatment) or SII plus EPZ5676 (E; 2 μM) and DZNep (Z) using the four-stage protocol.

    Pinometostat purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358.  [Abstract]

    Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.

    Pinometostat purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Jun 2;9(22):eadc9273.  [Abstract]

    H3K79me2 levels in HCI-H460 cells expressing WT or R231Q DOT1L after treatment with different concentrations (0, 0.5, and 5 μM, 9 days) of DOT1Lis (SGC0946, EPZ004777, and EPZ5676).

    Pinometostat purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2016 Aug 31;16(1):700.  [Abstract]

    Pharmacological inhibition of DOT1L induces E-cadherin and CD24 expression in MDA-MB-231 in vitro. Cells are treated with dose effects of EPZ-5676 (0.1 μM, 1 μM, 10 μM) or 0.1 % DMSO for the indicated days, followed by mRNA extraction and RT-qPCR with specific primers.
    • 生物活性

    • プロトコル

    • 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

    Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

    IC50 & Target

    DOT1L

     

    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    7 nM
    Compound: EPZ-5676
    Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
    Inhibition of DOT1L in human HeLa cells assessed as reduction in H3K79me2 level after 72 hrs by ELISA
    [PMID: 28337327]
    K562 IC50
    31 μM
    Compound: EPZ5676
    Anticancer activity against human K562 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    Anticancer activity against human K562 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    [PMID: 35612819]
    KOPN-8 IC50
    0.06 μM
    Compound: EPZ5676
    Anticancer activity against human KOPN-8 cells harbouring MLL-ENL assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    Anticancer activity against human KOPN-8 cells harbouring MLL-ENL assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 EC50
    0.004 μM
    Compound: 23, EPZ-5676
    Antiproliferative activity against human MOLM13 cells containing MLL-AF9
    Antiproliferative activity against human MOLM13 cells containing MLL-AF9
    [PMID: 23879463]
    MOLM-13 IC50
    0.03 μM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 IC50
    21 nM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 9 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 9 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 IC50
    227 nM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 4 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 4 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 IC50
    59 nM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 7 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 7 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 IC50
    73 nM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 6 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 6 days measured by CCK-8 kit method
    [PMID: 35612819]
    MOLM-13 IC50
    97 nM
    Compound: EPZ5676
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 5 days measured by CCK-8 kit method
    Anticancer activity against human MOLM-13 cells harbouring MLL-AF9 assessed as inhibition of cell growth treated for 5 days measured by CCK-8 kit method
    [PMID: 35612819]
    MV4-11 EC50
    0.004 μM
    Compound: 23, EPZ-5676
    Antiproliferative activity against human MV4-11 cells containing MLL-AF4
    Antiproliferative activity against human MV4-11 cells containing MLL-AF4
    [PMID: 23879463]
    MV4-11 IC50
    0.05 μM
    Compound: EPZ5676
    Anticancer activity against human MV4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    Anticancer activity against human MV4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    [PMID: 35612819]
    MV4-11 IC50
    15 nM
    Compound: EPZ-5676
    Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
    Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 treated for 6 hrs measured after 8 days by Celltiter-Glo reagent based assay
    [PMID: 28337327]
    MV4-11 IC50
    3 nM
    Compound: 38, EPZ-5676
    Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method
    Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method
    [PMID: 25406853]
    MV4-11 IC50
    3.5 nM
    Compound: 38, EPZ-5676
    Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assay
    Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assay
    [PMID: 25406853]
    RS4-11 IC50
    0.07 μM
    Compound: EPZ5676
    Anticancer activity against human RS4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    Anticancer activity against human RS4-11 cells assessed as inhibition of cell growth treated for 8 days measured by CCK-8 kit method
    [PMID: 35612819]
    THP-1 EC50
    0.004 μM
    Compound: 23, EPZ-5676
    Antiproliferative activity against human THP1 cells containing MLL-AF9
    Antiproliferative activity against human THP1 cells containing MLL-AF9
    [PMID: 23879463]
    体外実験

    Pinometostat (EPZ-5676) inhibits H3K79me2 with IC50 values of 3 nM and 5 nM in MV4-11 and HL60 cells, respectively. Pinometostat (EPZ-5676) is a potent inhibitor of MV4-11 proliferation with an IC50 value of 3.5 nM[1]. Pinometostat (EPZ-5676) induces a synergistic and durable antiproliferative effect, increases expression of differentiation markers and apoptosis as single agent, and demonstrates combination benefit in combination with AML standard of care drugs in MLL-r cells[2].

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

    体内実験

    Pinometostat (EPZ-5676) (70 mg/kg, i.p.) causes complete and sustained regression in a rat xenograft model of MLL-rearranged leukemia. Pinometostat (EPZ-5676) (70, 35 mg/kg, i.v.) reduces HOXA9 and MEIS1 mRNA levels of tumors taken from rats, and reduces MLL-fusion target gene expression in vivo[1].

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

    臨床実験
    分子量

    562.71

    分子式

    C30H42N8O3

    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    NC1=NC=NC2=C1N=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN([C@@H]4C[C@H](CCC5=NC6=C(C=CC(C(C)(C)C)=C6)N5)C4)C(C)C)O3

    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 : 100 mg/mL (177.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 100 mg/mL (177.71 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7771 mL 8.8856 mL 17.7711 mL
    5 mM 0.3554 mL 1.7771 mL 3.5542 mL
    10 mM 0.1777 mL 0.8886 mL 1.7771 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    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)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

    ×
    体積 (終了)

    V2

    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: ≥ 2.5 mg/mL (4.44 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.

      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: ≥ 2.5 mg/mL (4.44 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.

      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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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.
    純度とドキュメンテーション

    純度: 99.99%

    参考文献
    細胞実験
    [1]

    To analyse inhibition of histone methylation in MV4-11 cells following Pinometostat treatment, extracted histones (400 ng) are fractionated on a 10-20% Tris HCl gels with Tris-Glycine SDS running buffer under denaturing conditions and transferred to nitrocellulose filters. Filters are cut into strips and incubated for 1 hour in blocking buffer at room temperature (RT) and then incubated overnight at 4°C in blocking buffer. Filters are washed 3 times for 5 minutes with wash buffer (Phosphate buffered saline (PBS) including 0.01% Tween 20 (PBST)) and incubated with infrared tagged secondary antibody at RT for 1 hour. Filters are washed in PBST and reprobed for 1 hour at RT with the appropriate total histone antibody control (mouse anti-histone H3 (1:20,000), CST 3638, or mouse anti-histone H4 (1:10,000), CST 2935). Filters are washed again in PBST and incubated with infrared tagged secondary antibody (IRDye 800Cw donkey-anti-mouse IgG (1:20,000), Li-Cor 926-32212) at RT for 1 hour. After a final ish in PBST, filters are scanned using the Odyssey infared imager (Li-cor). To analyse inhibition of H3K79 methylation in peripheral blood mononuclear cells (PBMCs) from rats dosed with Pinometostat (EPZ-5676), 20 μL of PBMC whole cell lysate is fractionated on denaturing gels and analysed by immunoblotting with antibodies to H3K79me2 or total H3. Signal intensities specific for the H3K79me2 antibody and total histone H3 control antibody are quantified using Odyssey software. The H3K79me2 signal intensity is normalized by dividing it by the total histone H3 control signal intensity in the same lane.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    0.2 mL of a MV4-11 cell suspension (1×107 cells) in PBS is injected subcutaneously into female athymic nude mice (Crl:NU(Ncr)-Foxn1nu). Tumors are measured by calipers and mice are randomized according to tumor size into treatment groups (n=10) before the initiation of dosing with Pinometostat (EPZ-5676) when tumor volumes reache approximately 100 mma3. Pinometostat is administered intraperitoneally three times daily for 28 days at 10 and 20 mg/kg in 10% ethanol in saline. Mice are weighed and tumors measured with calipers twice weekly until the end of the study.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    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 / Ethanol 1 mM 1.7771 mL 8.8856 mL 17.7711 mL 44.4279 mL
    5 mM 0.3554 mL 1.7771 mL 3.5542 mL 8.8856 mL
    10 mM 0.1777 mL 0.8886 mL 1.7771 mL 4.4428 mL
    15 mM 0.1185 mL 0.5924 mL 1.1847 mL 2.9619 mL
    20 mM 0.0889 mL 0.4443 mL 0.8886 mL 2.2214 mL
    25 mM 0.0711 mL 0.3554 mL 0.7108 mL 1.7771 mL
    30 mM 0.0592 mL 0.2962 mL 0.5924 mL 1.4809 mL
    40 mM 0.0444 mL 0.2221 mL 0.4443 mL 1.1107 mL
    50 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8886 mL
    60 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7405 mL
    80 mM 0.0222 mL 0.1111 mL 0.2221 mL 0.5553 mL
    100 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4443 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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.

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    カスタマ需要量 *

    お名前 *

     

    タイトル

    メールアドレス *

     

    電話番号 *

    デパートメント

     

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

         

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Pinometostat
    製品番号:
    HY-15593
    数量:
    MCE 日本正規代理店: