123134-61-2
中文名稱
1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮
英文名稱
1-(2-Aminophenyl)-3-(3-nitrophenyl)-2-propen-1-one
CAS
123134-61-2
分子式
C15H12N2O3
分子量
268.27
MOL 文件
123134-61-2.mol
更新日期
2025/01/01 20:20:33
123134-61-2 結(jié)構(gòu)式
基本信息
中文別名
1-(2-氨基苯基)-3-(3-硝基苯基)-2-丙烯-1-酮1-(2-氨基苯基)-3-(3-硝基苯基)丙-2-烯-1-酮
英文別名
BIATMBIM6 antagonist-1
β-(2,5-Dihydro-5-oxoisoxazole-2-yl)-L-alanine
2-Propen-1-one, 1-(2-aminophenyl)-3-(3-nitrophenyl)-
(2S)-3-[(2,5-Dihydro-5-oxoisoxazole)-2-yl]-2-aminopropanoic acid
物理化學(xué)性質(zhì)
沸點(diǎn)482.1±45.0 °C(Predicted)
密度1.315±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 50 mg/mL (186.38 mM)
酸度系數(shù)(pKa)-0.47±0.10(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
TMBIM6 antagonist-1 是一個(gè)有潛力的 TMBIM6 拮抗劑，抑制 TMBIM6 與 mTORC2 結(jié)合，降低 mTORC2 活性，調(diào)節(jié)TMBIM6 釋放 Ca2+。體外研究
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. |
體內(nèi)研究
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. |