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EI1 Sale

(Synonyms: 6-氰基-N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-1-(1-乙基丙基)-1H-吲哚-4-甲酰胺,KB-145943) 目录号 : GC14756

A selective inhibitor of EZH2

EI1 Chemical Structure

Cas No.:1418308-27-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥893.00
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5mg
¥756.00
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10mg
¥1,386.00
现货
25mg
¥2,531.00
现货
50mg
¥3,990.00
现货
100mg
¥5,229.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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.

产品描述

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

Cas No. 1418308-27-6 SDF
别名 6-氰基-N-[(1,2-二氢-4,6-二甲基-2-氧代-3-吡啶基)甲基]-1-(1-乙基丙基)-1H-吲哚-4-甲酰胺,KB-145943
化学名 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
分子式 C23H26N4O2 分子量 390.48
溶解度 ≥ 19.5mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.561 mL 12.8048 mL 25.6095 mL
5 mM 0.5122 mL 2.561 mL 5.1219 mL
10 mM 0.2561 mL 1.2805 mL 2.561 mL
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