CMLD-2 |
رقم الكتالوجGC61567 |
CMLD-2 ، وهو مثبط لتفاعل HuR-ARE ، يربط بشكل تنافسي بروتين HuR مما يعطل تفاعله مع العناصر الغنية بالأدينين يوريدين (ARE) - التي تحتوي على mRNAs (Ki = 350 نانومتر)CMLD-2 يحث على موت الخلايا المبرمج يظهر نشاطًا مضادًا للورم في خلايا سرطانية مختلفة مثل خطوط خلايا سرطان القولون والبنكرياس والغدة الدرقية والرئةHu antigen R (HuR) هو بروتين مرتبط بالـ RNA ، يمكنه تنظيم استقرار mRNAs المستهدفة وترجمتها
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Cas No.: 958843-91-9
Sample solution is provided at 25 µL, 10mM.
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation[1][2].
CMLD-2 (1-75 μM; 24-72 h) inhibits thyroid cancer cell viability[2].CMLD-2 (20-30 μM; 24-48 h) activates caspases and induces apoptotic cell death in H1299 and A549 cells[3].CMLD-2 (30 μM; 24-48 h) induces G1 cell cycle arrest and mitochondrial perturbation in H1299 and A549 cell[3].CMLD-2 (30 μM; 24-48 h) reduces expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells[3].CMLD-2 (35 μM; 72 h) decreases directional migration capability in SW1736, 8505C, BCPAP and K1 cells. CMLD-2 induces a strong decrease of MAD2 mRNA levels in SW1736, 8505C, BCPAP and K1 cells[2]. Cell Viability Assay[2] Cell Line: SW1736, 8505C, BCPAP and K1 cells
[1]. Wu X, et, al. Identification and validation of novel small molecule disruptors of HuR-mRNA interaction. ACS Chem Biol. 2015 Jun 19;10(6):1476-84. [2]. Allegri , et, al. The HuR CMLD-2 inhibitor exhibits antitumor effects via MAD2 downregulation in thyroid cancer cells. Sci Rep. 2019 May 14;9(1):7374. [3]. Muralidharan R, et, al. HuR-targeted small molecule inhibitor exhibits cytotoxicity towards human lung cancer cells. Sci Rep. 2017 Aug 30;7(1):9694.
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