1. Epigenetics
  2. Histone Methyltransferase
  3. LLY-507

LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.

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

LLY-507 Chemical Structure

LLY-507 Chemical Structure

CAS No. : 1793053-37-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 139 In-stock
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10 mg USD 198 In-stock
25 mg USD 429 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LLY-507 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes[1].

    IC50 & Target[1]

    SMYD2

    <15 nM (IC50)

    In Vitro

    LLY-507 is >100-fold selective for SMYD2 over 21 other methyltransferases including SMYD3[1].
    LLY-507 binds to the substrate channel of SMYD2 and supports the selectivity of its inhibition[1].
    LY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC50 of 31 nM[1].
    LLY-507 (0.03-20 μM; 28 hours) inhibits SMYD2-mediated methylation of p53 Lys370 in U2OS cells, with an IC50 of 0.6 μM[1].
    LLY-507 (0-20 μM; 3-7 days) inhibits the proliferation of several ESCC, HCC, and breast cancer cell lines[1].

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

    Cell Proliferation Assay[1]

    Cell Line: ESCC, HCC, breast cancer cell lines
    Concentration: 0-20 μM
    Incubation Time: 3 days, 7 days
    Result: Inhibited tumor cell proliferation.

    Western Blot Analysis[1]

    Cell Line: HEK293 cells
    Concentration: 0.03 μM, 0.07 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM
    Incubation Time: 28 hours
    Result: Inhibited SMYD2-mediated methylation of p53 Lys370 in cells.
    Molecular Weight

    574.76

    Formula

    C36H42N6O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC(C2=CC=CC=C2N3CCN(CCN4C=C(C)C5=C4C=CC=C5)CC3)=CC(C#N)=C1)NCCCN6CCCC6

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 15 mg/mL (26.10 mM; Need ultrasonic and warming; 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 1.7399 mL 8.6993 mL 17.3986 mL
    5 mM 0.3480 mL 1.7399 mL 3.4797 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (4.35 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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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    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
    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, 6 months; -20°C, 1 month. 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 1.7399 mL 8.6993 mL 17.3986 mL 43.4964 mL
    5 mM 0.3480 mL 1.7399 mL 3.4797 mL 8.6993 mL
    10 mM 0.1740 mL 0.8699 mL 1.7399 mL 4.3496 mL
    15 mM 0.1160 mL 0.5800 mL 1.1599 mL 2.8998 mL
    20 mM 0.0870 mL 0.4350 mL 0.8699 mL 2.1748 mL
    25 mM 0.0696 mL 0.3480 mL 0.6959 mL 1.7399 mL
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    LLY-507 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.

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    Product Name:
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    Cat. No.:
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