1. Epigenetics
  2. Histone Methyltransferase
  3. EED226

EED226 

Cat. No.: HY-101117 Purity: 98.82%
Handling Instructions

EED226 est un inhibiteur du complexe répressif polycombique 2 (PRC2), qui se lie à la poche K27me3 lors du développement de l'ectoderme embryonnaire (EED) et présente une forte activité antitumorale dans le modèle de souris xénogreffe. EED226 est un inhibiteur d'EED puissant, sélectif et biodisponible par voie orale. EED226 inhibe PRC2 avec un IC50 de 23,4 nM lorsque le peptide H3K27me0 est utilisé comme substrat dans les tests enzymatiques in vitro.

EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.

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

EED226 Chemical Structure

EED226 Chemical Structure

CAS No. : 2083627-02-3

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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    EED226 purchased from MCE. Usage Cited in: ACS Infect Dis. 2020 Jul 10;6(7):1719-1733.

    2D10 cells are treated with various concentrations and times of EED226 and A-395, resulting in a dose- and time-dependent decrease in H3K27me3 as compared to controls UNC5679 and A-395N.
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    Description

    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model[1]. EED226 is a potent, selective, and orally bioavailable EED inhibitor[2]. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays[3].

    IC50 & Target

    IC50: 23.4 nM (PRC2)[3]

    In Vitro

    EED226 is a highly potent, efficient and selective inhibitor of EZH2 and EZH1 evaluated against a broad range of epigenetic and non-epigenetic targets. It potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation. EED226 has moderate permeability as the measured in Caco-2 cells at A→B=3.0x10-6 cm/s, with an efflux ratio at 7.6[2].
    In the in vitro enzymatic assays, EED226 inhibited PRC2 with an IC50 of 53.5 nM when the mononucleosome is used as the substrate, with the stimulatory H3K27me3 added at 1× Kact (1.0 μM)[3].

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

    In Vivo

    EED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model. In CD-1 mice, dosing of EED226 for 14 days at 300 mg/kg bid is well tolerated with no apparent adverse effects. It has very low in vivo clearance, and approximately 100% oral bioavailability. EED226 has low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB)[2].

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

    Molecular Weight

    369.40

    Formula

    C₁₇H₁₅N₅O₃S

    CAS No.

    2083627-02-3

    SMILES

    O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O

    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 : ≥ 29 mg/mL (78.51 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7071 mL 13.5355 mL 27.0709 mL
    5 mM 0.5414 mL 2.7071 mL 5.4142 mL
    10 mM 0.2707 mL 1.3535 mL 2.7071 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 (6.77 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (6.77 mM); Suspended solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [2]

    Mice: EED226 is formulated as a suspension in 0.5% PHMC+0.5% Tween 80 in water and administered orally by gavage at a dose volume of 10 mL/kg to the tumor bearing mice. At the end point, the animals is given the first dose administration. For PK analysis 100 μL of blood samples are collected from each animal by orbital sinus bleeding. For analysis of compound levels and PD in tissues, tumors are collected 4 hr post treatment and frozen immediately in liquid nitrogen. Tumor and body weight change data are analyzed statistically[2].

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

    References

    Purity: 98.82%

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    Keywords:

    EED226EED 226EED-226Histone MethyltransferasePRC2K27me3EEDantitumorInhibitorinhibitorinhibit

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    Product Name:
    EED226
    Cat. No.:
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