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HLI373 dihydrochloride

Catalog No. T36733 CAS 1782531-99-0

HLI373 dihydrochloride is a potent Hdm2 inhibitor, efficiently restraining the ubiquitin ligase activity of Hdm2 and effectively prompting apoptosis in DNA-damaging agent-sensitive tumor cells[1]. Additionally, HLI373 dihydrochloride exhibits antimalarial activity[2].

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HLI373 dihydrochloride Chemical Structure

HLI373 dihydrochloride, CAS 1782531-99-0

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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

Molecular Weight	414.33
Formula	C18H25Cl2N5O2
CAS No.	1782531-99-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

HLI373 dihydrochloride 1782531-99-0 HLI 373 HLI373 Dihydrochloride HLI-373 Dihydrochloride HLI-373 dihydrochloride HLI373 HLI-373 HLI 373 Dihydrochloride inhibitor inhibit

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