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502137-98-6

中文名称 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
英文名称 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
CAS 502137-98-6
分子式 C18H23N5O2
分子量 341.41
MOL 文件 502137-98-6.mol
502137-98-6 结构式 502137-98-6 结构式

基本信息

中文别名
化合物 T22087
英文别名
HLI 373
Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione, 5-[[3-(dimethylamino)propyl]amino]-3,10-dimethyl-
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride

物理化学性质

储存条件Desiccate at RT
溶解度<37.79mg/ml in H2O;insoluble in DMSO
形态固体
颜色Cream

常见问题列表

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。
靶点

Hdm2; Apoptosis; Antimalarial

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.
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