HLI373

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HLI373 

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。

HLI373

HLI373 Chemical Structure

CAS No. : 502137-98-6

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生物活性

HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents[1]. Antimalarial activity[2].

IC50 & Target

Hdm2[1]; Apoptosis[1]; Antimalarial[2]

体外研究
(In Vitro)

HLI373 (3-15 μM; 15 hours) selectively kills tumor cells harboring 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 IC50 values (below 6 μM) against both chloroquine-sensitive P. falciparum D6 strain (PfD6) and chloroquine-resistant P. falciparum W2 strain (PfW2) 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C18H23N5O2

CAS 号

502137-98-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Jirouta Kitagaki, et al. Targeting Tumor Cells Expressing p53 With a Water-Soluble Inhibitor of Hdm2. Mol Cancer Ther. 2008 Aug;7(8):2445-54.

    [2]. Jagrati Jain, et al. Inhibitors of Ubiquitin E3 Ligase as Potential New Antimalarial Drug Leads. BMC Pharmacol Toxicol. 2017 Jun 2;18(1):40.

    [3]. Ying Chen, et al. MDM2 Promotes Epithelial-Mesenchymal Transition and Metastasis of Ovarian Cancer SKOV3 Cells. Br J Cancer. 2017 Oct 10;117(8):1192-1201.

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