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CMLD-2 Sale

目录号 : GC61567

CMLD-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。

CMLD-2 Chemical Structure

Cas No.:958843-91-9

规格 价格 库存 购买数量
5 mg
¥2,700.00
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10 mg
¥4,500.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

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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