Antipsychotic agent 54

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Telomerase-IN-1 是一个端粒酶抑制剂，IC50 值为 0.19 μM。

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.

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.

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Cell Cycle/DNA Damage

Telomerase

Telomerase

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666859-49-0

386.42

C21H23FN2O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (258.79 mM; 超声助溶 )

COC(CN1CCC(CC1)C(=O)c1ccc(F)cc1)c1ccc(cc1)[N+]([O-])=O

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(-20℃)

With Ice Pack

≥ 2 years