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

LLY-507 

Cat. No.: HY-19313 Purity: 98.59%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 126 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.
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    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].

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

    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.

    Western Blot Analysis[1]

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

    574.76

    Formula

    C₃₆H₄₂N₆O

    CAS No.

    1793053-37-8

    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)

    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
    10 mM 0.1740 mL 0.8699 mL 1.7399 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    LLY-507LLY507LLY 507Histone MethyltransferasebreastcancerepigeneticsproteinmethylationSMYD2methyltransferasep53Inhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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