958843-91-9
中文名稱
958843-91-9
英文名稱
5,7-dimethoxy-8-(1-(4-methoxyphenyl)-3-oxo-3-(pyrrolidin-1-yl)propyl)-4-phenyl-2H-chromen-2-one
CAS
958843-91-9
分子式
C31H31NO6
分子量
513.58
MOL 文件
958843-91-9.mol
更新日期
2024/11/19 11:04:27
958843-91-9 結(jié)構(gòu)式
基本信息
中文別名
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 英文別名
5,7-dimethoxy-8-[1-(4-methoxyphenyl)-3-oxo-3-pyrrolidin-1-ylpropyl]-4-phenylchromen-2-one5,7-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)
所屬類別
生物化工：抑制劑物理化學性質(zhì)
儲存條件-20°C儲存
溶解度DMSO: 50 mg/mL (97.36 mM)
形態(tài)Solid
顏色White to off-white
InChIKeyPROGRNRRJJYCNX-UHFFFAOYSA-N
SMILESC1(=O)OC2=C(C(C3=CC=C(OC)C=C3)CC(=O)N3CCCC3)C(OC)=CC(OC)=C2C(C2=CC=CC=C2)=C1
常見問題列表
生物活性
CMLD-2 是一種 HuR-ARE 相互作用 的抑制劑。CMLD-2 競爭性結(jié)合 HuR 蛋白，破壞其與富含腺嘌呤-尿苷元素 (ARE) 的 mRNA 靶標的相互作用 (Ki=350 nM)。CMLD-2 可誘導凋亡并在結(jié)腸癌，胰腺癌，甲狀腺癌和肺癌細胞系中表現(xiàn)出抗腫瘤活性。Hu 抗原 R (HuR) 是一種 RNA 結(jié)合蛋白，可以調(diào)節(jié)靶標 mRNA 的穩(wěn)定性和翻譯。靶點
HuR
體外研究
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. |