5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
- CAS号:502137-98-6
- 英文名:5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
- 中文名:5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
- CBNumber:CB02518923
- 分子式:C18H23N5O2
- 分子量:341.41
- MOL File:502137-98-6.mol
- 储存条件 :Desiccate at RT
- 溶解度 :<37.79mg/ml in H2O;insoluble in DMSO
- 形态 :solid
- 颜色 :Cream
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride性质、用途与生产工艺
- 生物活性 HLI373 是一种有效的 Hdm2 抑制剂。HLI373 抑制 Hdm2 泛素连接酶活性。HLI373 可有效诱导肿瘤细胞 (对 DNA 破坏剂敏感的) 凋亡 (apoptosis)。具有抗疟疾 (antimalarial) 活性。
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靶点
Hdm2; Apoptosis; Antimalarial
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体外研究
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.
- 更新日期:2023/03/20
- 产品编号:HY-108640
- 产品名称:5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride HLI373
- CAS编号:502137-98-6
- 包装:5mg
- 价格:7500元
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