產(chǎn)品屬性：
產(chǎn)品名稱(chēng) | 規(guī)格 | CAS號(hào) | 型號(hào) |
EI1 | 10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg 100mg | 1418308-27-6 | EY-Y0165374 |
Cas No.1418308-27-6
別名
化學(xué)名 6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
分子式 C23H26N4O2
分子量 390.48
溶解度 ≥ 19.5mg/mL in DMSO
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)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.
關(guān)鍵字： 1418308-27-6;C23H26N4O2;EI1;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷(xiāo)售企業(yè)，公司自成立以來(lái)，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運(yùn)用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類(lèi)大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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