CMLD-2 |
| Katalog-Nr.GC61567 |
CMLD-2, ein Inhibitor der HuR-ARE-Wechselwirkung, bindet kompetitiv an das HuR-Protein, wodurch seine Wechselwirkung mit Adenin-Uridin-reichen Elementen (ARE)-enthaltenden mRNAs (Ki = 350 nM) unterbrochen wird. CMLD-2 induziert Apoptose und zeigt AntitumoraktivitÄt in verschiedenen Krebszellen wie Dickdarm-, BauchspeicheldrÜsen-, SchilddrÜsen- und Lungenkrebs-Zelllinien. Hu-Antigen R (HuR) ist ein RNA-bindendes Protein, das die StabilitÄt und Translation von Ziel-mRNAs regulieren kann.
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Cas No.: 958843-91-9
Sample solution is provided at 25 µL, 10mM.
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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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