1. Apoptosis
    Anti-infection
  2. MDM-2/p53
    Parasite
    Apoptosis
  3. HLI373 dihydrochloride

HLI373 dihydrochloride 

Cat. No.: HY-108640A
Handling Instructions

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

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HLI373 dihydrochloride Chemical Structure

HLI373 dihydrochloride Chemical Structure

CAS No. : 1782531-99-0

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Description

HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride 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]

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].

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.
Molecular Weight

414.33

Formula

C₁₈H₂₅Cl₂N₅O₂

CAS No.

1782531-99-0

SMILES

O=C1N=C2N(C)C3=C(C=CC=C3)C(NCCCN(C)C)=C2C(N1C)=O.[H]Cl.[H]Cl

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Keywords:

HLI373HLI 373HLI-373MDM-2/p53ParasiteApoptosisHdm2ubiquitinligaseactivityapoptosistumorcellsAntimalarialp53embryofibroblastInhibitorinhibitorinhibit

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HLI373 dihydrochloride
Cat. No.:
HY-108640A
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