Halofuginone

Synonyms: RU-19110

Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.

Halofuginone Chemical Structure

Halofuginone Chemical Structure

CAS: 55837-20-2

Selleck's Halofuginone has been cited by 8 publications

Purity & Quality Control

Batch: S814401 DMSO] 8 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.81%
99.81

Halofuginone Related Products

Choose Selective DNA/RNA Synthesis Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HuH7 Antiplasmodial assay 1 hr Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay, IC50=0.017μM. 23701465
Click to View More Cell Line Experimental Data

Biological Activity

Description Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
Targets
Smad3 [2] prolyl-tRNA synthetase [1]
(Cell-free assay)
18.3nM(Ki)
In vitro
In vitro In mammals, halofuginone at 10 ng/ml down-regulates Smad3, blocking TGF-β signaling and preventing both the differentiation of fibroblasts to myofibroblasts and the transitioning of epithelial cells to mesenchymal cells[2].
Kinase Assay Assay of ProRS activity
The prolyl tRNA synthetase domain of human EPRS (ProRS) is expressed in E.coli with a 6-his tag and purified. Enzymatic activity is assayed using incorporation of 3H Pro into the tRNA fraction essentially, except that the charged tRNA fraction is isolated by rapid batchwise binding to Mono Q sepharose and quantitated by liquid scintillation counting. For all kinetic assays, the concentration of active enzyme in the reaction is 40 nM. Similar inhibition by HF is seen using the human ProRS domain purified from bacteria and full length EPRS purified from rat liver.
Cell Research Cell lines primary murine CD4+ CD25− T cells/MEFs
Concentrations 5-20nM
Incubation Time 4 or 24hrs
Method

Primary murine CD4+ CD25− T cells are activated through the TCR in Th17 polarizing conditions in the presence of either 10nM MAZ1310 or HF and amino acid supplements. Th17 differentiation is assayed in the absence or presence of HF or borrelidin, with or without 1 mM threonine or proline supplementation. MEFs are treated with or without HF (50 nM) and/or Proline (2 mM) for 4 hours (CHOP, S100A4) or 24 hours (ColIA1, Col1A2). 

Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 22393274
Western blot PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 p15 / p21 / E-cadherin / MMP2 / MMP9 / MMP14 / CD44 c-IAP / Mcl-1 p-JNK / JNK / p-p38 / p38 ATG7 26015407
In Vivo
In vivo Halofuginone clearly extends the survival times of the parasite-infected mice. Oral treatment with halofuginone at doses of 0.2 and 1 mg/kg has an apparent curative effect for the infected mice. The subcutaneous administration of 0.2 mg of halofuginone per kg likewise extends the survival times of the infected mice, but none of the mice is cured. The mice in the 5-mg/kg dose groups die before the completion of treatment with the drug either orally or subcutaneously. Subcutaneous treatment with halofuginone appears to be more toxic to mice than oral treatment[3].
Animal Research Animal Models 4- to 5-week-old ICR mice
Dosages 0.2 and 1 mg/kg
Administration Oral treatment/subcutaneous administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting
Cirrhosis Liver
University of Texas Southwestern Medical Center|National Cancer Institute (NCI)
July 2024 Phase 2
NCT06156761 Not yet recruiting
Breast Cancer
Cancer Institute and Hospital Chinese Academy of Medical Sciences|CSPC Ouyi Pharmaceutical Co. Ltd.
November 28 2023 Not Applicable
NCT05778617 Not yet recruiting
Parkinson Disease
University College London
September 2023 Phase 3
NCT06122012 Recruiting
Diabetic Peripheral Neuropathic Pain
Haisco Pharmaceutical Group Co. Ltd.
May 1 2023 Not Applicable
NCT02630121 Recruiting
Sleep Apnea|Chronic Nasal Congestion
University of South Florida
April 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 414.68 Formula

C16H17BrClN3O3

CAS No. 55837-20-2 SDF Download Halofuginone SDF
Smiles C1CC(C(NC1)CC(=O)CN2C=NC3=CC(=C(C=C3C2=O)Cl)Br)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 8 mg/mL ( (19.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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