HLI373
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. Antimalarial activity.
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- CAS No.: 502137-98-6
- Formule: C18H23N5O2
- Masse moléculaire:341.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild type p53 mouse embryo fibroblasts (MEFs), and p53-deficient MEFs
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Concentration:3, 10, 15 μM
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Incubation Time:15 hours
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Result:Increased cell death in wild type p53 MEFs in a dose-dependent manner, p53-deficient MEFs were relatively resistant.
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Cell Line:U2OS cells
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Concentration:5, 10 μM
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Incubation Time:8 hours
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Result:Blocked p53 degradation caused by co-transfection with plasmids encoding p53 and Hdm2.
Chemical Information
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CAS No. 502137-98-6
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Masse moléculaire 341.41
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Formule C18H23N5O2
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SMILES
O=C1N=C2N(C)C3=C(C=CC=C3)C(NCCCN(C)C)=C2C(N1C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HLI373 Related Classifications
HY-108640 Related Classifications
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