Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HLI373 是一种有效的 Hdm2抑制剂, Hdm2 是一种泛素连接酶(E3)。HLI373 可有效诱导肿瘤细胞 (对 DNA 破坏剂敏感的) 凋亡 (apoptosis),并且具有抗疟疾 (antimalarial) 活性。
产品描述 | HLI373 is an efficacious Hdm2 inhibitor. Hdm2 is an ubiquitin ligase (E3). HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents [1]. HLI 373 also shows prominent antimalarial activity [2]. |
体外活性 | HLI373 (3-15 μM; 15 hours) selectively kills tumor cells expressing wild type p53 [1]. HLI373 (10-50 μM) stabilizes cellular Hdm2 in a dose-dependent manner. HLI373 (3 μM) activates p53 transcription [1]. HLI373 selectively inhibits auto-ubiquitylation of Hdm2 [1]. 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 [1]. 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 [2]. 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 [3]. Cell Viability Assay [1] 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 [1] 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. |
分子量 | 341.41 |
分子式 | C18H23N5O2 |
CAS No. | 502137-98-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
HLI 373 502137-98-6 HLI-373 HLI373 Inhibitor inhibitor inhibit