5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
![5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 结构式](https://img.chemicalbook.com/CAS/20180808/GIF/502137-98-6.gif)
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 性质
| 储存条件 | Desiccate at RT |
|---|---|
| 溶解度 | <37.79mg/ml，水中；不溶于 DMSO |
| 形态 | 固体 |
| 颜色 | 淡黄色，米色 |
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 用途与合成方法
Hdm2; Apoptosis; Antimalarial
HLI373 (3-15 μM; 15 hours) selectively kills tumor cells harboring wild type p53.
HLI373 (10-50 μM) stabilizes cellular Hdm2 in a dose-dependent manner.
HLI373 (3 μM) activates p53 transcription.
HLI373 selectively inhibits auto-ubiquitylation of Hdm2.
Co-transfection with plasmids encoding p53 and Hdm2 results in degradation of p53. Incubation with HLI373 (5-10 μM; 8 hours) blocks p53 degradation. HLI373 increases p53 and Hdm2 protein levels in cells.
HLI 373 also shows lower IC
50
values (below 6 μM) against both chloroquine-sensitive
P. falciparum
D6 strain (
Pf
D6) and chloroquine-resistant
P. falciparum
W2 strain (
Pf
W2) and exhibits early growth inhibition.
HLI-373 is a MDM2 inhibitor interrupting its ubiquitin E3 ligase activity, could abolish the ubiquitylation of its substrate protein p53. HLI-373 targets the C-terminus functioning as an E3 ubiquitin ligase.
Cell Viability Assay
| Cell Line: | Wild type p53 mouse embryo fibroblasts (MEFs), and p53-deficient MEFs |
| Concentration: | 3, 10, 15 μM |
| Incubation Time: | 15 hours |
| Result: | Increased cell death in wild type p53 MEFs in a dose-dependent manner, p53-deficient MEFs were relatively resistant. |
Western Blot Analysis
| Cell Line: | U2OS cells |
| Concentration: | 5, 10 μM |
| Incubation Time: | 8 hours |
| Result: | Blocked p53 degradation caused by co-transfection with plasmids encoding p53 and Hdm2. |
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2023-03-20 | HY-108640 | 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride | 502137-98-6 | 5mg | 7500 |
