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EI1 EZH2 inhibitor

Catalog No.B1021
Size Price Stock Qty
10mM (in 1mL DMSO)
$130.00
In stock
5mg
$105.00
In stock
10mg
$180.00
In stock
25mg
$335.00
In stock
50mg
$540.00
In stock
100mg
$699.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

EI1

Protocol

Cell experiment [1]:

Cell lines

Ezh2 mutant diffused large B-cell lymphoma (DLBCL) cells, Ezh2 wild-type DLBCL cells and mouse embryonic fibroblasts (MEFs)

Preparation method

The solubility of this compound in DMSO is > 19.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

10 μM; 11 ~ 15 days

Applications

In DLBCL cells, EI1 inhibited the methylation of cellular lysine 27 of histone H3 (H3K27), and up-regulated the expression of Ezh2 target gene p16. In MEFs, EI1 inhibited H3K27me3 and cell proliferation. In DLBCL cells carrying Ezh2 mutation, EI1 selectively inhibited cell growth, as well as induced cell cycle arrest and apoptosis.

References:

[1]. Qia W, Chan HM, Teng L, Li L, Chuai S, Zhang RP, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfiob O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen ZJ, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P and Li E. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci. 2012 Dec; 109(52): 213605.

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Chemical Properties

Cas No. 1418308-27-6 SDF Download SDF
Chemical Name 6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
Canonical SMILES CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C
Formula C23H26N4O2 M.Wt 390.48
Solubility >19.5mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

IC50: A potent and selective suppressor of Ezh2 with IC50 values of 15 nM and 13 nM for wild type Ezh2 and Ezh2 Y641F mutant, respectively

EI1 performs as a highly potent inhibitor of Ezh2 which is named enhancer of zeste homolog 2. Mutation and over-expression of Ezh2 has been linked to the development of cancer. Since Ezh2 is upregulated in multiple cancers, it seems to play a crucial role in the regulation of tumor angiogenesis and has been considered as a potential target in anticancer therapy. Ezh2 stimulates cancer development by inhibiting tumor-suppressing genes. Suppressing Ezh2 activity may therefore inhibit tumor growth. [1]

In vitro: Based on studies from DLBCL cells, it was shown that EI1 suppressed cellular H3K27 methylation and activated expression of Ezh2 target gene - p16. EI1 also blocked H3K27 methylation and cell proliferation in mouse embryonic fibroblasts. In addition, EI1 potently and selectively inhibited the growth of DLBCL cells carrying Ezh2 mutation, and therefore resulted in cell cycle arrest and apoptosis. [1]

In vivo: So far, no in vivo study has been conducted.

Clinical trial: So far, no clinical trial has been conducted.

Reference:
[1]Qia W, Chan HM, Teng L, Li L, Chuai S, Zhang RP, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfiob O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen ZJ, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P and Li E.  Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci. 2012 Dec; 109(52): 213605.