958843-91-9
| 中文名称 | 958843-91-9 |
|---|---|
| 中文同义词 | 5,7-二甲氧基-8-[1-(4-甲氧基苯基)-3-氧代-3-(1-吡咯烷基)丙基]-4-苯基-2H-1-苯并吡喃-2-酮;5,7-二甲氧基-8-(1-(4-甲氧苯基)-3-氧亚基-3-(吡咯烷-1-基)丙基)-4-苯基-2H-色烯-2-酮;5,7-二甲氧基-8-(1-(4-甲氧基苯基)-3-氧代-3-(吡咯烷基-1-基)丙基)-4-苯基-2H-苯并吡喃-2-酮 |
| 英文名称 | 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one |
| 英文同义词 | 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one;5,7-dimethoxy-8-[1-(4-methoxyphenyl)-3-oxo-3-pyrrolidin-1-ylpropyl]-4-phenylchromen-2-one;5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one(WXC05487);2H-1-Benzopyran-2-one, 5,7-dimethoxy-8-[1-(4-methoxyphenyl)-3-oxo-3-(1-pyrrolidinyl)propyl]-4-phenyl-;CMLD 2,CMLD2 |
| CAS号 | 958843-91-9 |
| 分子式 | C31H31NO6 |
| 分子量 | 513.58094 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 958843-91-9.mol |
| 结构式 |  |
958843-91-9 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亚砜：50 mg/ml（97.36 mM） |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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。
HuR
CMLD-2 (1-75 μM; 24-72 h) inhibits thyroid cancer cell viability.
CMLD-2 (20-30 μM; 24-48 h) activates caspases and induces apoptotic cell death in H1299 and A549 cells.
CMLD-2 (30 μM; 24-48 h) induces G1 cell cycle arrest and mitochondrial perturbation in H1299 and A549 cell.
CMLD-2 (30 μM; 24-48 h) reduces expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells.
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.
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 Analysis
| Cell 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. |