EED-226 | PRC2 methyltransferase inhibitor

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°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$85.00
25 mg$285.00
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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

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°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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

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