CMLD-2 |
カタログ番号GC61567 |
HuR-ARE 相互作用の阻害剤である CMLD-2 は、競合的に HuR タンパク質に結合し、アデニン-ウリジン リッチ エレメント (ARE) を含む mRNA (Ki=350 nM) との相互作用を破壊します。 CMLD-2 誘導アポトーシスは、結腸、膵臓、甲状腺、および肺癌細胞株などのさまざまな癌細胞で抗腫瘍活性を示します。 Hu 抗原 R (HuR) は RNA 結合タンパク質であり、標的 mRNA の安定性と翻訳を調節できます。
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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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