HLI 373 - CAS 502137-98-6
Category: Inhibitor
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Apoptosis Inducer
HLI 373 is an inhibitor of Hdm2 ubiquitin ligase (E3) that blocks Hdm2-mediated ubiquitylation and proteasomal degradation of p53 and activates p53-dependent transcription. HLI 373 has a therapeutic effect in several tumor cell lines that express wild-type p53 such as LOX-IMVI, A549, HT1080 and U2OS.
Brife Description:
Hdm2 ubiquitin ligase (E3) inhibitor
≥99% by HPLC
HLI373; HLI-373; HLI 373; NSC-373989; NSC 373989; NSC373989. 5-[[3-Dimethylamino)propyl]amino]-3,10-dimethylpyrimido[4,5-b]quinoline-2,4(3H,10H)-dione dihydrochloride
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1.Inhibitors of ubiquitin E3 ligase as potential new antimalarial drug leads.
Jain J;Jain SK;Walker LA;Tekwani BL BMC Pharmacol Toxicol. 2017 Jun 2;18(1):40. doi: 10.1186/s40360-017-0147-4.
BACKGROUND: ;Protein ubiquitylation is an important post-translational regulation, which has been shown to be necessary for life cycle progression and survival of Plasmodium falciparum. Ubiquitin is a highly conserved 76 amino acid polypeptide, which attaches covalently to target proteins through combined action of three classes of enzymes namely, the ubiquitin-activating enzyme (E1), ubiquitin-conjugating enzyme (E2) and ubiquitin-protein ligase (E3). Ubiquitin E1 and E2 are highly conserved within eukaryotes. However, the P. falciparum E3 ligase is substantially variable and divergent compared to the homologs from other eukaryotes, which make the E3 ligase a parasite-specific target.;METHODS: ;A set of selected E3 ubiquitin ligase inhibitors was tested in vitro against a chloroquine-sensitive P. falciparum D6 strain (PfD6) and a chloroquine-resistant P. falciparum W2 strain (PfW2). The inhibitors were also tested against Vero and transformed THP1 cells for cytotoxicity. The lead antimalarial E3 ubiquitin ligase inhibitors were further evaluated for the stage-specific antimalarial action and effects on cellular development of P. falciparum in vitro. Statistics analysis was done by two-way ANOVA followed by Tukey and Sidak multiple comparison test using GraphPad Prism 6.
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CAS 502137-98-6 HLI 373

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