1. Epigenetics
  2. Histone Methyltransferase


Cat. No.: HY-101117 Purity: 98.70%
Handling Instructions

EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.

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

EED226 Chemical Structure

EED226 Chemical Structure

CAS No. : 2083627-02-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.

IC50 & Target

IC50: 22 nM (EED226)[1]

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[1].

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)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 29 mg/mL (78.51 mM)

*"≥" means soluble, but saturation unknown.

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.
Animal Administration

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[1].

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

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Purity: 98.70%

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Cat. No.: HY-101117