生物活性 靶点 体外研究 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 试剂级价格
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ChemicalBook  CAS数据库列表  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

生物活性 靶点 体外研究 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 试剂级价格
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride,502137-98-6,结构式
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
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride化学性质
  • 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。
  • 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.
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
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride 试剂级价格
  • 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
5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dionedihydrochloride生产厂家
  • 公司名称：MedBio脉铂医药
  • 联系电话：021-69568360 18916172912
  • 电子邮件：order@med-bio.cn
  • 国家：中国
  • 产品数：8141
  • 优势度：58
  • 公司名称：TargetMol中国（陶术生物）
  • 联系电话： 4008200310
  • 电子邮件：marketing@tsbiochem.com
  • 国家：中国
  • 产品数：24017
  • 优势度：58
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