Art. -Nr.: HY-101117

EED226

16 Cited Publications

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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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Reinheit: 99.56%
CAS. Nr.: 2083627-02-3
Formel: C₁₇H₁₅N₅O₃S
Molecular Weight:369.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

EED226 Chemical Structure

CAS. Nr.: 2083627-02-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
G-401	IC₅₀	85 μM Compound: EED226	Anticancer activity against human G-401 cells assessed as cell growth inhibition Anticancer activity against human G-401 cells assessed as cell growth inhibition	[PMID: 36724635]
KARPAS-422	GI₅₀	0.08 μM Compound: EED226; 1	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	[PMID: 35352560]
KARPAS-422	IC₅₀	0.08 μM Compound: 43	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	[PMID: 28092155]
KARPAS-422	IC₅₀	0.18 μM Compound: 4; EED226	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	[PMID: 32580550]
KARPAS-422	IC₅₀	125.4 nM Compound: 6; EED226	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	[PMID: 34613724]
KARPAS-422	IC₅₀	80 nM Compound: 7; EED226	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	[PMID: 35093670]

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× K_act (1.0 μM)^[3].

MedChemExpress (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 EZH2^MUT 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 t_1/2 (2.2 h), and moderate plasma protein binding (PPB)^[2].

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

Chemical Information

CAS. Nr. 2083627-02-3
Appearance Solid
Molecular Weight 369.40
Formel C₁₇H₁₅N₅O₃S
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (16)

All Cell Proliferation/Viability AssayWB

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Journal Impact Factor

Cancer Cell

Whole-genome doubling drives immune evasion by silencing antigen presentation. [Abstract]

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

Drug addiction unveils a repressive methylation ceiling in EZH2-mutant lymphoma. [Abstract]

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.
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.
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

Nucleation and spreading maintain Polycomb domains every cell cycle. [Abstract]

2024 Apr 23;43(4):114090. PMID: 38607915
Stem Cell Reports

An innovative in vitro system unveils IGF1R signaling regulating Merkel cell generation. [Abstract]

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.
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
Res Sq

2025 Dec 17.
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
bioRxiv

2024 October 02.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.77 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.

Working Solution

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.

Protocol 1

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

EED226

16 Cited Publications

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EED226

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) EED226

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EED226

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) EED226

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EED226 Related Classifications

HY-101117 Related Classifications