1. Epigenetics
  2. Histone Methyltransferase
  3. EPZ005687

EPZ005687 

Cat. No.: HY-15555 Purity: 99.49%
Handling Instructions

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

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

EPZ005687 Chemical Structure

EPZ005687 Chemical Structure

CAS No. : 1396772-26-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1  mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    EPZ005687 purchased from MCE. Usage Cited in: Sci Rep. 2016 Aug 19;6:29176.

    EZH2 level induced by IL-1β is decreased following pretreatment with the EZH2 inhibitor EPZ005687 (5.6 μM), with a concomitant upregulation of SOX9 (P < 0.05). (A) The normal chondrocytes (P2) are treated with IL-1β (10 ng/mL) for 24 hours to induce chondrocyte pathological change followed by knockdown by siEZH2 or treatment by pharmacological inhibitor EPZ005687. The effect of each treatment is investigated by Western-blotting and quantitative analysis (B,C).

    EPZ005687 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Mar 16;108:280-299.

    SFRP-1 expression is significantly inhibited by EZH2-EGFP and enhanced by siEZH2 or EZH2 inhibitor EPZ005687.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

    IC50 & Target[1]

    EZH2

    24 nM (Ki)

    In Vitro

    EPZ005687 shows concentration-dependent inhibition of PRC2 enzymatic activity with an IC50 value of 54±5 nM. EPZ005687 specifically inhibits H3K27 methylation in lymphoma cells. EPZ005687 has a notable effect on proliferation of the EZH2Y641F-bearing cell line. EPZ005687 decreases proliferation in mutant but not wild-type EZH2 lymphoma cells[1]. EPZ005687 (0.5, 1, 5 and 10 µM) induces an obvious apoptosis of U937 cells in a dose-dependent manner. EPZ005687 inhibits obviously the proliferation of U937 cells but has weak effect on the proliferation of NBMCD34+ cells. EPZ005687 induces G1 phase blocking and decreases the percentage of cells in S phase in U937 cells. In addition, EPZ005687 produces obviously depletion of H3K27 methylation in U937 cells, but hardly has effect on the H3K27 methylation of NBMCD34+ cells[2].

    Molecular Weight

    539.67

    Formula

    C₃₂H₃₇N₅O₃

    CAS No.

    1396772-26-1

    SMILES

    O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6

    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 : 9.4 mg/mL (17.42 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8530 mL 9.2649 mL 18.5298 mL
    5 mM 0.3706 mL 1.8530 mL 3.7060 mL
    10 mM 0.1853 mL 0.9265 mL 1.8530 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: ≥ 1.67 mg/mL (3.09 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1.67 mg/mL (3.09 mM); Clear solution

    • 3.

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

      Solubility: ≥ 1.67 mg/mL (3.09 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    10-point curves of EPZ005687 are made using serial 3-fold dilution in DMSO, beginning at 2.5 mM (final top concentration of compound is 50 μM and the DMSO is 2%). A 1 μL aliquot the inhibitor dilution series is spotted in a 384-well microtiter plate. The 100% inhibition control consisted of 1 mM final concentration of the product inhibitor S-adenosylhomocysteine (SAH). Compound is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween 20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction. Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, then transferred to 384-well Flashplate and washed after 30 min.

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

    Cell Assay
    [1]

    For cell cycle, WSU-DLCL2 cells are plated in 12-well plates at a density of 1×105 cells per mL. Cells are incubated with EPZ005687 at 0.2 μM, 0.67 μM, 2 μM and 6 μM, in a total of 2 mL, over a course of 10 d. All remaining cell cycle analysis is performed.

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

    References

    Purity: 99.49%

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    Keywords:

    EPZ005687EPZ 005687EPZ-005687Histone MethyltransferaseInhibitorinhibitorinhibit

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    Product name:
    EPZ005687
    Cat. No.:
    HY-15555
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