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958843-91-9

中文名稱(chēng) 958843-91-9
英文名稱(chēng) 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 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-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)
所屬類(lèi)別
生物化工:抑制劑

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)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

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見(jiàn)問(wèn)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(jìng)爭(zhēng)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(biāo)的相互作用 (Ki=350 nM)。CMLD-2 可誘導(dǎo)凋亡并在結(jié)腸癌,胰腺癌,甲狀腺癌和肺癌細(xì)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(biāo) mRNA 的穩(wěn)定性和翻譯。
靶點(diǎn)

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.
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