CMLD012612 |
| カタログ番号GC62698 |
CMLD012612 は、ヒドロキサメート基を含むアミジノロカグレートであり、強力な真核生物開始因子 4A (eIF4A) 阻害剤です。 CMLD012612 は細胞翻訳を阻害し、NIH/3T3 細胞に対して 2 nM の IC50 値で細胞毒性を示します。 CMLD012612 は、RNA ヘリカーゼ (eIF4A) の挙動を変更することによって真核生物の翻訳開始を阻害し、強力な抗腫瘍活性を持っています。
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Cas No.: 2368900-35-8
Sample solution is provided at 25 µL, 10mM.
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CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1].
The IC50 of CMLD012612 toward NIH/3T3 cells is 2 nM. The primary mechanism of action of CMLD012612 is dependent on eIF4A1, since eIF4A1em1jp cells are at least 10-fold more resistant than parental NIH/3T3 cells. The sensitivity of eIF4A1em1jp cells to CMLD012612 observed at higher concentrations may be due to the presence of wild-type eIF4A2 in the cells[1].
CMLD012612 (0.5 mg/kg; intraperitoneal injection; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection, indicating inhibitory activity toward protein synthesis[1].When administered to mice bearing myr-Akt/Em-Myc lymphomas, CMLD012612 (0.2 mg/kg; intraperitoneal injection; daily; for 5 days; female C57BL/6 mice) treatment effectively synergizes with Doxorubicin, leading to complete tumor loss[1].
[1]. Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593.
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