2. Epigenetics
  3. Histone Methyltransferase
  4. EPZ031686

EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research.

For research use only. We do not sell to patients.

EPZ031686 Chemical Structure

EPZ031686 Chemical Structure

CAS No. : 2095161-11-6

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1 mg USD 140 In-stock
5 mg USD 320 In-stock
10 mg USD 490 In-stock
50 mg USD 1450 In-stock
100 mg USD 2150 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

EPZ031686 Related Antibodies

Top Publications Citing Use of Products

    EPZ031686 purchased from MedChemExpress. Usage Cited in: Aging. 2020 Nov 3;12(21):21423-21445.  [Abstract]

    EPZ031686 (20 μM) reverses Ang II-induced PARP16 and RAECs senescence. Inhibition of Smyd3 could downregulate protein level of PARP16, together with reduced ER stress and senescence markers.

    View All Histone Methyltransferase Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EPZ031686 is an potent and orally active SMYD3 inhibitor and with an IC50 value of 3 nM. EPZ031686 can be used for cancer research[1].

    IC50 & Target[1]

    SMYD3

    3 nM (IC50)

    In Vivo

    EPZ031686 (1-50 mg/mL; p.o. and i.v.; Male CD-1 mice) has good bioavailability following oral dosing in mice[1].

    Pharmacokinetic Analysis in Male CD-1 mice[1]

    Route Dose (mg/kg) CL (mL/min/kg) CLr (mL/min/kg) Vss (L/kg) tmax (h) tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) AUCINF_obs (ng·h/mL)
    i.v. 1 27 5.3 2.3 1.7 / / 603 616
    p.o. 5 / / / 2.7/td> 0.89 345 1281 1479
    p.o. 50 / / / 2.2 1.3 4693 21158 21170

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

    591.09

    Formula

    C26H34ClF3N4O4S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C1)NC2=C1C=C(C(N[C@@H]3C[C@H]4N(S(CC5CCN(CCCC(F)(F)F)CC5)(=O)=O)[C@H](CC4)C3)=O)C(Cl)=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 35 mg/mL (59.21 mM; ultrasonic and warming and heat to 60°C; 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 1.6918 mL 8.4589 mL 16.9179 mL
    5 mM 0.3384 mL 1.6918 mL 3.3836 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
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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:  30% PEG300  70% (20% SBE-β-CD in Saline)

      Solubility: 10 mg/mL (16.92 mM); Suspended solution; Need ultrasonic and warming

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.75 mg/mL (2.96 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.5 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.
    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.
    Purity & Documentation

    Purity: 99.71%

    COA (251 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References

    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 1.6918 mL 8.4589 mL 16.9179 mL 42.2947 mL
    5 mM 0.3384 mL 1.6918 mL 3.3836 mL 8.4589 mL
    10 mM 0.1692 mL 0.8459 mL 1.6918 mL 4.2295 mL
    15 mM 0.1128 mL 0.5639 mL 1.1279 mL 2.8196 mL
    20 mM 0.0846 mL 0.4229 mL 0.8459 mL 2.1147 mL
    25 mM 0.0677 mL 0.3384 mL 0.6767 mL 1.6918 mL
    30 mM 0.0564 mL 0.2820 mL 0.5639 mL 1.4098 mL
    40 mM 0.0423 mL 0.2115 mL 0.4229 mL 1.0574 mL
    50 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8459 mL
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    EPZ031686 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.

    Keywords:

    EPZ0316862095161-11-6EPZ 031686EPZ-031686Histone MethyltransferaseSMYD3cancerbioavailabilityInhibitorinhibitorinhibit

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