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 IC 50 of 0.19 μM.

Solid

IC50: 0.19 μM (Telomerase)

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. has not indepe

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[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.

In Vitro: DMSO : 100 mg/mL (258.79 mM; Need ultrasonic)配制储备液