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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
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- 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
- 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
- 中文名:
- 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
- 中文别名:
- 化合物 T22087;化合物 HLI 373
- CBNumber:
- CB02518923
- 分子式:
- C18H23N5O2
- 分子量:
- 341.41
- MOL File:
- 502137-98-6.mol
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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride化学性质
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储存条件:
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Desiccate at RT
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溶解度:
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<37.79mg/ml in H2O;insoluble in DMSO
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形态:
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solid
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颜色:
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Cream
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水溶解性:
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water: 50mg/mL
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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
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。
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
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Cell Line:
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Wild type p53 mouse embryo fibroblasts (MEFs), and p53-deficient MEFs
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Concentration:
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3, 10, 15 μM
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Incubation Time:
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15 hours
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Result:
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Increased cell death in wild type p53 MEFs in a dose-dependent manner, p53-deficient MEFs were relatively resistant.
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Western Blot Analysis
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Cell Line:
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U2OS cells
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Concentration:
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5, 10 μM
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Incubation Time:
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8 hours
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Result:
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Blocked p53 degradation caused by co-transfection with plasmids encoding p53 and Hdm2.
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5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2023/03/20 | HY-108640 | 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
HLI373 | 502137-98-6 | 5mg | 7500元 |
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride
生产厂家
502137-98-6, 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 相关搜索:
- 抑制剂
- 高端化学
- C18H23N5O22HCl
- C18H23N5O2HCl
- 化合物 HLI 373
- 化合物 T22087
- 502137-98-6
- Pyrimido[4,5-b]quinoline-2,4(3H,10H)-dione, 5-[[3-(dimethylamino)propyl]amino]-3,10-dimethyl-
- HLI 373
- 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride