958843-91-9
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- CAS号:
- 958843-91-9
- 英文名:
- 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
- 英文别名:
- CMLD 2,CMLD2;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;2H-1-Benzopyran-2-one, 5,7-dimethoxy-8-[1-(4-methoxyphenyl)-3-oxo-3-(1-pyrrolidinyl)propyl]-4-phenyl-;5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one(WXC05487)
- 中文名:
- 958843-91-9
- 中文别名:
- 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;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
- CBNumber:
- CB83303827
- 分子式:
- C31H31NO6
- 分子量:
- 513.58094
- MOL File:
- 958843-91-9.mol
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958843-91-9化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 50 mg/mL (97.36 mM)
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形态:
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Solid
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颜色:
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White to off-white
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958843-91-9性质、用途与生产工艺
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 (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
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Cell Line:
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SW1736, 8505C, BCPAP and K1 cells
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Concentration:
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1, 5, 10, 25, 35, 50, 75 μM
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Incubation Time:
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24, 48, 72 hours
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Result:
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Reduced the viability of all the four cell lines when used at 35, 50 and 75 μM concentration and at different time points.
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Apoptosis Analysis
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Cell Line:
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H1299, A549, H1975, HCC827, MRC-9 and CCD16 cells
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Concentration:
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20, 30 μM
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Incubation Time:
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24, 48 hours
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Result:
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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.
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Cell Cycle Analysis
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Cell Line:
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H1299, A549, MRC-9 and CCD16 cells
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Concentration:
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30 μM
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Incubation Time:
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24, 48 hours
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Result:
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Induced greater G1 phase cell cycle arrest in H1299 and A549 cells than in MRC-9 and CCD16 cells.
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Western Blot Analysis
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Cell Line:
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H1299, A549, H1975, HCC827, CCD16 and MRC-9 cells
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Concentration:
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20, 30 μM
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Incubation Time:
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24, 48 hours
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Result:
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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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958843-91-9
上下游产品信息
上游原料
下游产品
958843-91-9, 958843-91-9 相关搜索:
- 抑制剂
- 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
- 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-(1-吡咯烷基)丙基]-4-苯基-2H-1-苯并吡喃-2-酮
- 958843-91-9
- CMLD 2,CMLD2
- 2H-1-Benzopyran-2-one, 5,7-dimethoxy-8-[1-(4-methoxyphenyl)-3-oxo-3-(1-pyrrolidinyl)propyl]-4-phenyl-
- 5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one(WXC05487)
- 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