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EED226

Catalog No. T3458   CAS 2083627-02-3

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
EED226 Chemical Structure
EED226, CAS 2083627-02-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 48.00
10 mg In stock $ 76.00
25 mg In stock $ 126.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.66%
Purity: 99.66%
Purity: 98.14%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
Targets&IC50 EED:22 nM
In vitro EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors. It regulates histone H3K27 methylation and PRC2 target gene expression in cells. In the in vitro enzymatic assays, EED226 inhibits PRC2 with an IC50 (half-maximal inhibitory concentration) of 23.4 nM when the H3K27me0 peptide is used as substrate and 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). EED226 is noncompetitive with both SAM and peptide substrate. EED226 bound to EED and PRC2 complex with a 1:1 stoichiometry and Kd of 82 nM and 114 nM, respectively. EED226 does not disrupt the PRC2 complex and could still occupy its binding pocket with a SAM-competitive EZH2 inhibitor bound to PRC2. EED226 shows remarkable selectivity for PRC2 complex over 21 other protein methyltransferases, kinases and other protein classes, The only other histone methyltransferase that can be inhibited by EED226 is the EZH1-PRC2 complex. EED226 with moderate permeability leads to a dose-dependent decrease of both global H3K27me3 and H3K27me2 markers in G401 cell[1].
In vivo EED226 effectively induces tumor regression in a mouse xenograft model. EED226 in a solid dispersion formulation are well tolerated in animals. EED226 clearly demonstrates a dose-dependent efficacy in the mouse xenograph study[1]. EED226 inhibits the growth of diffuse large B-cell lymphoma (DLBCL) xenografts and reduces H3K27me3 levels to a similar extent as an EZH2 inhibitor[2]. EED226 has very low in vivo and in vitro clearance and approximately 100% oral bioavailability, low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB)(14.4%). Its solubility is relatively low and with little dependency on the pH of the medium[3].
Cell Research G401 cells are treated with EED226 for 3 d at the indicated concentrations. Total histone H3 is shown as a loading control. WB analysis for protein expression of H3K27me3, H3K27me2, H3K27me1. (Only for Reference)
Molecular Weight 369.4
Formula C17H15N5O3S
CAS No. 2083627-02-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 68 mg/mL (184.1 mM)

TargetMolReferences and Literature

1. Qi W, et al. Nat Chem Biol. 2017, 13(4):381-388. 2. Cancer Discov. 2017, 7(4):OF8. doi: 10.1158/2159-8290.CD-RW2017-030. 3. Y Huang, et al. J Med Chem. 60 (6):2215-2226.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Bioactive Compound Library Methylation Compound Library Epigenetics Compound Library NO PAINS Compound Library Anti-Aging Compound Library Inhibitor Library Anti-Cancer Compound Library Orally Active Compound Library

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Keywords

EED226 2083627-02-3 Chromatin/Epigenetic Histone Methyltransferase inhibit antitumor EED 226 Inhibitor PRC2 EED K27me3 EED-226 inhibitor

 

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