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Telomerase-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telomerase-IN-1图片
CAS NO:666859-49-0
规格:98%
分子量:386.42
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Telomerase-IN-1是一个端粒酶抑制剂,IC50值为0.19μM.
CAS:666859-49-0
分子式:C21H23FN2O4
分子量:386.42
纯度:98%
存储:Store at -20°C

Background:

Telomerase-IN-1 is a Telomerase inhibitor with an IC50 of 0.19 μM.


Our in vitro studies show that title compound (Telomerase-IN-1) has high inhibitory activity against telomerase and high antiproliferative capacity on SMMC-7721 cells, and has no obvious toxic effect on human normal hepatocyte cells. Telomerase-IN-1 treatment decreases the growth of cancer cells in dose- and time-dependent manners; however, the viability of L-02 shows slight changes in the compound at 10 μM. 48 h of SMMC-7721 cell treatment with the Telomerase-IN-1 (20, 40, and 80 nM) causes increase of apoptosis. Forty-eight hours of SMMC-7721 cell treatment with the Telomerase-IN-1(20, 40, and 80 nM) causes significant accumulation of green fluorescence, indicating a decrease in MMP. At 40 nM, Telomerase-IN-1 significantly increases expressions of cyt-c and Bax, but the Bcl-2 level is decreased[1].


Our in vivo studies show that this compound (Telomerase-IN-1) significantly inhibits tumor growth in xenograft tumor models. Results show that endoplasmic reticulum stress (ERS) through ER over response (EOR) activates the expression of hTERT, and then induces ERS, which is believed to be intricately associated with oxidative stress and mitochondrial dysfunction, resulting in apoptotic cell death, thereby modulating the expression of downstream signaling molecules including CHOP (CAAT/enhancer-binding protein homologous protein)) and mitochondrion pathway of apoptosis, leading to inhibition of cell proliferation[1].


[1]. Cheng X, et al. Discovery of (4-bromophenyl)(3-hydroxy-4-methoxyphenyl)methanone through upregulating hTERT induces cell apoptosis and ERS. Cell Death Dis. 2017 Aug 24;8(8):e3016.