358721-70-7
中文名稱
UBCS039
英文名稱
UBCS039
CAS
358721-70-7
分子式
C16H13N3
分子量
247.29
MOL 文件
358721-70-7.mol
更新日期
2024/04/02 15:36:40
358721-70-7 結(jié)構(gòu)式
基本信息
中文別名
化合物UBCS0394-(吡啶-3-基)-4,5-二氫吡咯并[1,2-A]喹喔啉
英文別名
UBCS039Pyrrolo[1,2-a]quinoxaline, 4,5-dihydro-4-(3-pyridinyl)-
所屬類別
有機原料：雜環(huán)化合物物理化學性質(zhì)
沸點453.9±45.0 °C(Predicted)
密度1.25±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO : 125 mg/mL (505.48 mM)
酸度系數(shù)(pKa)4.66±0.12(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
UBCS039是第一個合成的SIRT6激活劑，EC50為38 μM，在多種人類腫瘤細胞系中均可誘導自噬的時間依賴性激活。靶點
| Target | Value |
|
SIRT6
(Cell-free assay) | 38 μM(EC50) |
體外研究
UBCS039 (75 μM, 48 or 72 hours) induces deacetylation of SIRT6-targeted histone H3 sites in human cancer cells.
UBCS039 leads to autophagosome accumulation in human cancer cells.
UBCS039 induces autophagy via AMP-activated protein kinase (AMPK) signaling pathway activation.
Western Blot Analysis
| Cell Line: | Human H1299 cells. |
| Concentration: | 75 μM. |
| Incubation Time: | 48 and 72 hours. |
| Result: | Induced deacetylation of SIRT6-targeted histone H3 sites in human H1299 cells. |
Western Blot Analysis
| Cell Line: | Human H1299 cells. |
| Concentration: | 75 μM. |
| Incubation Time: | 48 and 72 hours. |
| Result: | Induced deacetylation of SIRT6-targeted histone H3 sites in human H1299 cells. |
Cell Proliferation Assay
| Cell Line: | Human H1299 cells. |
| Concentration: | 100 μM. |
| Incubation Time: | 48 and 72 hours. |
| Result: | Led to a strong decrease of cell proliferation in a dose-dependent manner when compared with control or DMSO-treated cells, starting from day 3 of growth (48 h after treatment) in both H1299 and HeLa cell lines. |