Reagents and instruments for immunology, cell biology and molecular biology.

EED226 [2083627-02-3]

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Cat# HY-101117-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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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]

Cellular Effect

Cell Line	Type	Value	Description	References
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.

Solvent & Solubility

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.

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

View the 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.

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

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

Purity & Documentation

Purity: 99.56%

Data Sheet (280 KB) SDS (392 KB)

COA (250 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[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]

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EED226 [2083627-02-3]

Cat# HY-101117-1ml

Brand : MedChemExpress

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