EED226
Based on 16 publication(s) in Google Scholar
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.
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- Pureza: 99.56%
- No. CAS: 2083627-02-3
- Fòrmula: C17H15N5O3S
- Peso molecular:369.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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HY-L226
Publications Citing Use of MedChemExpress (MCE) EED226
More- Cancer Cell. 2026 May 7:S1535-6108(26)00218-7. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
- Adv Sci (Weinh). 2026 Jun 16:e19359. [Abstract]
- Cell Death Dis. 2022 Feb 15;13(2):155. [Abstract]
- Genome Biol. 2020 Aug 6;21(1):195. [Abstract]
- Cell Rep. 2024 Apr 23;43(4):114090. [Abstract]
- Stem Cell Reports. 2025 Dec 26:102756. [Abstract]
- Sci Rep. 2020 Sep 16;10(1):15201. [Abstract]
- iScience. 2023 Jun 7;26(7):107035. [Abstract]
- ACS Infect Dis. 2020 Jul 10;6(7):1719-1733. [Abstract]
- Front Oncol. 2019 Jan 14:8:679. [Abstract]
- PLoS One. 2024 Jun 3;19(6):e0298965. [Abstract]
- Res Sq. 2025 Dec 17.
- bioRxiv. 2025 Sep 18:2025.09.16.676613. [Abstract]
- bioRxiv. 2024 October 02.
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
IC50: 23.4 nM (PRC2)[3]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| G-401 | IC50 |
85 μM
Compound: EED226
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Anticancer activity against human G-401 cells assessed as cell growth inhibition
Anticancer activity against human G-401 cells assessed as cell growth inhibition
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[PMID: 36724635] |
| KARPAS-422 | GI50 |
0.08 μM
Compound: EED226; 1
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Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 mutant assessed as inhibition of cell growth after 14 days by beckman coulter counting method
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[PMID: 35352560] |
| KARPAS-422 | IC50 |
0.08 μM
Compound: 43
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Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method
Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method
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[PMID: 28092155] |
| KARPAS-422 | IC50 |
0.18 μM
Compound: 4; EED226
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Growth inhibition of human KARPAS422 cells incubated for 7 days by WST8 assay
Growth inhibition of human KARPAS422 cells incubated for 7 days by WST8 assay
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[PMID: 32580550] |
| KARPAS-422 | IC50 |
125.4 nM
Compound: 6; EED226
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Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
Growth inhibition of human KARPAS-422 cells assessed as cell growth incubated for 7 days by lactate dehydrogenase based WST-8 assay
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[PMID: 34613724] |
| KARPAS-422 | IC50 |
80 nM
Compound: 7; EED226
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Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant incubated for 14 days
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant incubated for 14 days
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[PMID: 35093670] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2083627-02-3
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Appearance Solid
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Peso molecular 369.40
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Fòrmula C17H15N5O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2026 May 7:S1535-6108(26)00218-7. PMID: 42102810 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Chem Biol
2023 Sep;19(9):1105-1115. PMID: 36973442
EED226 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Dose-response proliferation curves of Karpas-422 wild-type under EED226 (0.01-10 μM; 10 d) treatment.
EED226 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
EED226 (1-10 μM; 72 h) reduced H3K27me3 levels in wild-type and CXCdel+/− Karpas-422 cells.
EED226 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Dose-response proliferation curves of Karpas-422 CXCdel+/− under EED226 (0.01-10 μM) treatment.
EED226 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Sep;19(9):1105-1115. [Abstract]
Bar plots of cell viability following transduction of individual EZH2 sgRNAs and treatment with EED226 (1 μM; 6 weeks) in Karpas-422 cells.
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Adv Sci (Weinh)
PRC2.1 Coordinates Peri-Nucleolar H3K27me3-Enriched Heterochromatin Organization and NPM1 Pentamerization to Maintain Nucleolar Integrity. [Abstract]2026 Jun 16:e19359. PMID: 42299771 -
Cell Death Dis
Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer. [Abstract]2022 Feb 15;13(2):155. PMID: 35169119
EED226 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 15;13(2):155. [Abstract]
EED226 (0.04-10 μM; 72 h) dose-dependently inhibited cellular H3K27me3 in HeLa cells.
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Genome Biol
The RNA-binding protein SERBP1 functions as a novel oncogenic factor in glioblastoma by bridging cancer metabolism and epigenetic regulation. [Abstract]2020 Aug 6;21(1):195. PMID: 32762776 -
Cell Rep
2024 Apr 23;43(4):114090. PMID: 38607915 -
Stem Cell Reports
2025 Dec 26:102756. PMID: 41455470 -
Sci Rep
A membrane transporter determines the spectrum of activity of a potent platinum-acridine hybrid anticancer agent. [Abstract]2020 Sep 16;10(1):15201. PMID: 32939009 -
iScience
Polycomb repressive complex 2 binds and stabilizes NANOG to suppress differentiation-related genes to promote self-renewal. [Abstract]2023 Jun 7;26(7):107035. PMID: 37448562 -
ACS Infect Dis
Evaluation of EED Inhibitors as a Class of PRC2-Targeted Small Molecules for HIV Latency Reversal. [Abstract]2020 Jul 10;6(7):1719-1733. PMID: 32347704
EED226 purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2020 Jul 10;6(7):1719-1733. [Abstract]
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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Front Oncol
Aspirin Inhibits Natural Killer/T-Cell Lymphoma by Modulation of VEGF Expression and Mitochondrial Function. [Abstract]2019 Jan 14:8:679. PMID: 30693272 -
PLoS One
Age-dependent regulation of ELP1 exon 20 splicing in Familial Dysautonomia by RNA Polymerase II kinetics and chromatin structure. [Abstract]2024 Jun 3;19(6):e0298965. PMID: 38829854 -
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bioRxiv
Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]2025 Sep 18:2025.09.16.676613. PMID: 41000734 -
Solvente y solubilidad
DMSO : ≥ 125 mg/mL (338.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 0.5% HPMC/1% Tween-80 in Saline water
Solubility: 10 mg/mL (27.07 mM); Suspened solution; Need ultrasonic
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li L, et al. Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED. PLoS One. 2017 Jan 10;12(1):e0169855. [Content Brief]
[2]. Huang Y, et al. Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy. J Med Chem. 2017 Mar 23;60(6):2215-2226. [Content Brief]
[3]. Qi W, et al. An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol. 2017 Apr;13(4):381-388. [Content Brief]
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 | 2.7071 mL | 13.5355 mL | 27.0709 mL | 67.6773 mL |
| 5 mM | 0.5414 mL | 2.7071 mL | 5.4142 mL | 13.5355 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7071 mL | 6.7677 mL | |
| 15 mM | 0.1805 mL | 0.9024 mL | 1.8047 mL | 4.5118 mL | |
| 20 mM | 0.1354 mL | 0.6768 mL | 1.3535 mL | 3.3839 mL | |
| 25 mM | 0.1083 mL | 0.5414 mL | 1.0828 mL | 2.7071 mL | |
| 30 mM | 0.0902 mL | 0.4512 mL | 0.9024 mL | 2.2559 mL | |
| 40 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6919 mL | |
| 50 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3535 mL | |
| 60 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1280 mL | |
| 80 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2707 mL | 0.6768 mL |
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