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HLI 373

Catalog No. T22087 CAS 502137-98-6

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].

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HLI 373, CAS 502137-98-6

Pack Size	Availability	Price/USD	Quantity
25 mg	6-8 weeks	$ 1,627.00
50 mg	6-8 weeks	$ 2,438.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description

In vitro

HLI373, at concentrations ranging from 3-15 μM over 15 hours, preferentially induces cell death in tumor cells harboring wild type p53, according to study [1]. At higher doses (10-50 μM), it dose-dependently stabilizes Hdm2, while a lower concentration of 3 μM activates p53 transcription. This compound effectively blocks the auto-ubiquitylation of Hdm2 and, when cells are co-transfected with p53 and Hdm2, HLI373 can prevent the degradation of p53, especially at 5-10 μM after 8 hours of treatment. Moreover, it increases both p53 and Hdm2 protein levels in cells. Notably, HLI373 demonstrates potent activity against both chloroquine-sensitive and resistant strains of P. falciparum, displaying IC50 values below 6 μM and inducing early growth inhibition. Functioning as an MDM2 inhibitor by targeting its C-terminus, HLI373 disrupts the ubiquitin E3 ligase activity of MDM2, which is key to the ubiquitylation of p53, highlighting its potential in cancer therapy. In cell viability assays, it was shown to cause increased cell death in wild type p53 mouse embryo fibroblasts (MEFs) in a dose-dependent manner, whereas p53-deficient MEFs exhibited resistance. Western blot analyses revealed that the compound prevents p53 degradation in U2OS cells when co-transfected with p53 and Hdm2 encoding plasmids.

Molecular Weight	341.41
Formula	C18H23N5O2
CAS No.	502137-98-6

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

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

HLI 373 502137-98-6 HLI-373 HLI373 inhibitor inhibit

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