CMLD-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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=350 nM)。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, 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.

Cell Viability Assay Cell Line:SW1736, 8505C, BCPAP and K1 cells Concentration:1, 5, 10, 25, 35, 50, 75 μM Incubation Time:24, 48, 72 hours Result:Reduced the viability of all the four cell lines when used at 35, 50 and 75?μM concentration and at different time points.Apoptosis AnalysisCell Line:H1299, A549, H1975, HCC827, MRC-9 and CCD16 cells Concentration:20, 30 μM Incubation Time:24, 48 hours Result:Marked activated the caspase-9 and -3 in lung tumor cells.Induce the cleavage of PARP in lung tumor cells.Significantly increased the annexin-V-positive staining in lung tumor cells.Cell Cycle Analysis Cell Line:H1299, A549, MRC-9 and CCD16 cells Concentration:30 μM Incubation Time:24, 48 hours Result:Induced greater G1 phase cell cycle arrest in H1299 and A549 cells than in MRC-9 and CCD16 cells.Western Blot Analysis Cell Line:H1299, A549, H1975, HCC827, CCD16 and MRC-9 cells Concentration:20, 30 μM Incubation Time:24, 48 hours Result:Diminished protein expression of HuR, Bcl-2, Cyclin E and Bcl-XL and increased expression of p27 and BAX in lung tumor cells.

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Apoptosis

Apoptosis

Apoptosis | HuR

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958843-91-9

513.58

C31H31NO6

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (97.36 mM; 超声助溶 )

COc1ccc(cc1)C(CC(=O)N1CCCC1)c1c(OC)cc(OC)c2c(cc(=O)oc12)-c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years