my account
Login
  Loading... Please wait...

Product Details

EED-226 | PRC2 methyltransferase inhibitor

EED-226 (2083627-02-3) is a potent (IC50 = 23.4 nM)  and selective allosteric inhibitor of the EED subunit of the methyltransferase polycomb repressive complex 2 (PRC2).1,2 It caused drastic proliferation inhibition in lymphoma cells with EZH2 mutations and caused shrinkage and slower tumor growth in mice using a subcutaneous xenograft model of Karpas422.

References/Citations
1) Huang et al. (2017), Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy; J. Med. Chem. 60 2215
2) Qi et al. (2017), An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED; Nat. Chem. Biol. 13 381

swipe
Image 1

Catalog#  10-4021-0005

$85.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
Request Bulk Quote
CAS:
2083627-02-3
Catalog Number:
10-4021
Activity:
PRC2 methyltransferase inhibitor
Chemical Name:
N-(Furan-2-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolol[4,3-c)pyrimidine-5-amine
Molecular Weight:
369.40
Molecular Formula:
C17H15N5O3S
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

Connect with Focus

Click the button below to add the EED-226 | PRC2 methyltransferase inhibitor to your wish list.