1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮
| 中文名称 | 1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮 |
|---|---|
| 中文同义词 | 1-(2-氨基苯基)-3-(3-硝基苯基)丙-2-烯-1-酮;1-(2-氨基苯基)-3-(3-硝基苯基)-2-丙烯-1-酮 |
| 英文名称 | 1-(2-Aminophenyl)-3-(3-nitrophenyl)-2-propen-1-one |
| 英文同义词 | (2S)-3-[(2,5-Dihydro-5-oxoisoxazole)-2-yl]-2-aminopropanoic acid;BIA;β-(2,5-Dihydro-5-oxoisoxazole-2-yl)-L-alanine;2-Propen-1-one, 1-(2-aminophenyl)-3-(3-nitrophenyl)-;TMBIM6 antagonist-1;1-(2-Aminophenyl)-3-(3-nitrophenyl)prop-2-en-1-one;TMBIM-6 antagonist-1,TMBIM6 antagonist 1,HT1080,SKBR3,TMBIM6 antagonist1,MCF7,Mammalian target of Rapamycin,TMBIM6 antagonist-1,Ca2+,Inhibitor,inhibit,mTOR,TMBIM6;1-(2-Aminophenyl)-3-(3-nitrophenyl)-2-propen-1-one |
| CAS号 | 123134-61-2 |
| 分子式 | C15H12N2O3 |
| 分子量 | 268.27 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 123134-61-2.mol |
| 结构式 |  |
1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮 性质
| 沸点 | 482.1±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.315±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：50 mg/mL（186.38 mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | -0.47±0.10(Predicted) |
| 颜色 | 浅黄至黄色 |
TMBIM6 antagonist-1 是一个有潜力的 TMBIM6 拮抗剂，抑制 TMBIM6 与 mTORC2 结合，降低 mTORC2 活性，调节TMBIM6 释放 Ca2+。
TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) significantly and dose-dependently inhibits cell viability in HT1080, MCF7, MDA-MB-2341 and SKBR3 cells, with IC
50
values of 1.7 ± 0.1 μM for HT1080, 2.6 ± 0.4 μM for MCF cells, 2.6 ± 0.5 μM for MDA-MB-231 cells, and 2.4 ± 0.4 μM for SKBR3 cells, respectively.
TMBIM6 antagonist-1 (BIA, 10 μM) treatment decreases cell migration in HT1080, MCF7, MDA-MB-231, and SKBR3 cells, not TMBIM6 KO HT1080 cells.
Cell Viability Assay
| Cell Line: | HT1080, MCF7, MDA-MB-2341 and SKBR3 cells. |
| Concentration: | 0.5-10 μM. |
| Incubation Time: | 3 days. |
| Result: | Inhibited cell viability. |
Western Blot Analysis
| Cell Line: | WT and TMBIM6 KO HT1080 cells. |
| Concentration: | 0, 2, 5 μM. |
| Incubation Time: | |
| Result: | Downregulated the protein levels of AKT-pS473. |
TMBIM6 antagonist-1 (1 mg/kg, IP 5 days per week during 25 days) significantly impaires cell-driven tumor growth.
| Animal Model: |
Six- to eight-week BklNbt:BALB/c/nu/nu old mice (HT1080 and MDA-MB-231 cells).
|
| Dosage: | 1 mg/kg. |
| Administration: | IP 5 days per week during 25 days. |
| Result: | Impaired cell-driven tumor growth. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-137175 | TMBIM6 antagonist-1 | 1 mg | 830元 | |
| 2024/08/19 | HY-137175 | 1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮 TMBIM6 antagonist-1 | 123134-61-2 | 5mg | 1950元 |