CMLD-2
目录号 : GC61567CMLD-2是一种HuR-ARE相互作用的抑制剂。CMLD-2竞争性结合HuR蛋白,破坏其与富含腺嘌呤-尿苷元素(ARE)的mRNA靶标的相互作用(Ki=350nM)。CMLD-2可诱导凋亡并在结肠癌,胰腺癌,甲状腺癌和肺癌细胞系中表现出抗肿瘤活性。Hu抗原R(HuR)是一种RNA结合蛋白,可以调节靶标mRNA的稳定性和翻译。
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.
Cas No. | 958843-91-9 | SDF | |
Canonical SMILES | O=C1C=C(C2=CC=CC=C2)C3=C(OC)C=C(OC)C(C(C4=CC=C(OC)C=C4)CC(N5CCCC5)=O)=C3O1 | ||
分子式 | C31H31NO6 | 分子量 | 513.58 |
溶解度 | DMSO: 50 mg/mL (97.36 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.9471 mL | 9.7356 mL | 19.4712 mL |
5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL |
10 mM | 0.1947 mL | 0.9736 mL | 1.9471 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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