2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. EPZ020411

EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer.

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CAS 番号 : 1700663-41-7

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5 mg $165 在庫あり
10 mg $275 在庫あり
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of EPZ020411:

EPZ020411 関連抗体

Top Publications Citing Use of Products

    EPZ020411 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413.  [Abstract]

    EPZ020411(PRMT6i; 200-1000 nM) in combination with GSK591(PRMT5i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

    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

    EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer[1][2].

    IC50 & Target

    PRMT6

    0.01 μM (IC50)

    PRMT1

    0.119 μM (IC50)

    PRMT8

    0.223 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    0.637 μM
    Compound: EPZ020411
    Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method
    Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method
    		[PMID: 26101569]
    A-375 IC50
    7.1 μM
    Compound: EPZ020411
    Inhibition of PRMT1 in human A375 cells assessed as effect on monomethyl R*GG motif methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method
    Inhibition of PRMT1 in human A375 cells assessed as effect on monomethyl R*GG motif methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method
    		[PMID: 26101569]
    HCC827 IC50
    4.15 μM
    Compound: EPZ020411
    Antiproliferative activity against human HCC827 cells for 7 days by MTT assay
    Antiproliferative activity against human HCC827 cells for 7 days by MTT assay
    		[PMID: 36566712]
    HCC827 IC50
    8.57 μM
    Compound: EPZ020411
    Antiproliferative activity against human HCC827 cells for 5 days by MTT assay
    Antiproliferative activity against human HCC827 cells for 5 days by MTT assay
    		[PMID: 36566712]
    HCC827 IC50
    > 100 μM
    Compound: EPZ020411
    Antiproliferative activity against human HCC827 cells for 3 days by MTT assay
    Antiproliferative activity against human HCC827 cells for 3 days by MTT assay
    		[PMID: 36566712]
    MDA-MB-435 IC50
    1.1 μM
    Compound: EPZ020411
    Antiproliferative activity against human MDA-MB-435 cells for 7 days by MTT assay
    Antiproliferative activity against human MDA-MB-435 cells for 7 days by MTT assay
    		[PMID: 36566712]
    MDA-MB-435 IC50
    90.43 μM
    Compound: EPZ020411
    Antiproliferative activity against human MDA-MB-435 cells for 5 days by MTT assay
    Antiproliferative activity against human MDA-MB-435 cells for 5 days by MTT assay
    		[PMID: 36566712]
    MDA-MB-435 IC50
    94.65 μM
    Compound: EPZ020411
    Antiproliferative activity against human MDA-MB-435 cells for 3 days by MTT assay
    Antiproliferative activity against human MDA-MB-435 cells for 3 days by MTT assay
    		[PMID: 36566712]
    体外実験

    EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
    EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].

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

    EPZ020411 関連抗体

    Western Blot Analysis[1]

    Cell Line: A375 cells
    Concentration: 0-20 μM
    Incubation Time: 24 hours
    Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM.

    Apoptosis Analysis[2]

    Cell Line: Cultured cochleae cells
    Concentration: 20-40 μM
    Incubation Time: 6 hours
    Result: Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Also reduced hair cell loss caused by cisplatin treatment.
    体内実験

    EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
    1.19 Pharmacokinetic Parameters of EPZ020411 in rats[1].

    Rats
    IV 1 mg/kg    		 Rats
    SC 5 mg/kg
    CL (mL/min/kg) 19.7±1.0
    Vss (L/kg) 11.1±1.6
    t1/2 (h) 8.54±1.43 9.19±1.60
    tmax (h) 0.444
    Cmax (ng/mL) 844±306
    AUC0-τ (h·ng/mL) 745±34 2456±135
    AUC0-inf (h·ng/mL) 846±45 2775±181
    F (%) 65.6±4.3

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

    Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity model[2]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 10 mg/kg once
    Result: Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
    分子量

    442.59

    分子式

    C25H38N4O3
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    DMSO : 4.76 mg/mL (10.75 mM; ultrasonic and adjust pH to 7 with 1 M HCl; 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 2.2594 mL 11.2971 mL 22.5943 mL
    5 mM 0.4519 mL 2.2594 mL 4.5189 mL
    10 mM 0.2259 mL 1.1297 mL 2.2594 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
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    ×
    Volume
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    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 (5.65 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 (5.65 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Saline

      Solubility: 4.5 mg/mL (10.17 mM); Clear solution; Need ultrasonic

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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: 98.07%

    COA (251 KB) HNMR (436 KB) RP-HPLC (257 KB) LCMS (94 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2594 mL 11.2971 mL 22.5943 mL 56.4857 mL
    5 mM 0.4519 mL 2.2594 mL 4.5189 mL 11.2971 mL
    10 mM 0.2259 mL 1.1297 mL 2.2594 mL 5.6486 mL
    • No file chosen (Maximum size is: 1024 Kb)
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    EPZ020411 Related Classifications

    • Molarity Calculator

    • Dilution 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:

    EPZ0204111700663-41-7EPZ 020411EPZ-020411Histone MethyltransferaseApoptosisoncologytool compoundcochleaeA375apoptosiscancerInhibitorinhibitorinhibit

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    製品名:
    EPZ020411
    製品番号:
    HY-12970
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