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EI1

现货
Catalog No.
B1021
EZH2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
5mg
¥ 1,050.00
现货
10mg
¥ 1,800.00
现货
25mg
¥ 3,350.00
现货
50mg
¥ 5,400.00
现货
100mg
¥ 6,990.00
现货

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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.

Chemical Properties

StorageStore at -20°C
M.Wt390.48
Cas No.1418308-27-6
FormulaC23H26N4O2
Solubility≥19.5mg/mL in DMSO
Chemical Name6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
SDFDownload SDF
Canonical SMILESCCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

含Ezh2突变的弥漫性大B细胞淋巴瘤 (DLBCL) 细胞、Ezh2野生型DLBCL细胞以及小鼠胚胎成纤维细胞 (MEFs)

制备方法

在DMSO中的溶解度大于19.5 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10 μM;11 ~ 15天

实验结果

在DLBCL细胞中,EI1抑制细胞组蛋白H3赖氨酸27 (H3K27) 甲基化,上调Ezh2靶基因p16表达。在MEFs中,EI1抑制H3K27me3和细胞增殖。在携带Ezh2突变的DLBCL细胞中,EI1选择性地抑制细胞生长,并诱导细胞周期停滞和细胞凋亡。

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.

质量控制

化学结构

EI1