Halofuginone

For research use only. Not for use in humans.

Catalog No.S8144

Halofuginone Chemical Structure

Molecular Weight(MW): 414.68

Halofuginone 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.

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Biological Activity

Description Halofuginone 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
prolyl-tRNA synthetase [1]
(Cell-free assay)
18.3nM(Ki)
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].

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 22393274     


Halofuginone is nontoxic at low concentrations. The viability of human corneal fibroblasts treated with halofuginone is similar to control for concentrations of 10 ng/ml or less. The viability of cells treated with 50 ng/ml or 100 ng/ml halofuginone is significantly decreased compared to control (* p<0.005). Viability is expressed as fluorescence intensity of metabolized resazurin relative to control (n=5, bar=S.E.M.).

22393274
Western blot
PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 ; 

PubMed: 26015407     


HOS cells (left panels) and U2OS cells (right panels) were treated with halofuginone as indicated for 24 hours. After incubation, Caspase-3 and PARP levels were detected by Western Blot analysis of whole cell lysates. Actin antibody was used as internal control. Representative blots of three experiments were shown.

p15 / p21 / E-cadherin / MMP2 / MMP9 / MMP14 / CD44 ; 

PubMed: 26884857     


Detection of p15, p21, E-cadherin, MMP2, MMP9, MMP14 and CD44 gene/protein expressions in HepG2 cells after treatment with different concentration of halofuginone. 

c-IAP / Mcl-1 ; 

PubMed: 26884857     


Detection of Mcl-1 and c-IAP gene/protein expressions in HepG2 cells after treatment with different concentration of halofuginone.

p-JNK / JNK / p-p38 / p38 ; 

PubMed: 26884857     


MAPK signaling pathway involves in halofuginone-mediated inhibition of HepG2 cells. A. The increased protein expressions of p-JNK in HepG2 after treatment with different concentration of halofuginone. B. The decreased protein expressions of p-p38 in HepG2 after treatment with different concentration of halofuginone.

ATG7; 

PubMed: 28492544     


Protein expression of ATG7 in HCT116 and SW480 cells (upper panel); quantitative analysis of protein expressions (bottom panel) treated with 0, 5, 10, 20 nM HF for 12 h in high-glucose medium. *P<0.05, **P<0.01. 

26015407 26884857 28492544
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].

Protocol

Kinase Assay:

[1]

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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:

[1]

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  • 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). 


    (Only for Reference)
Animal Research:

[4]

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  • Animal Models: 4- to 5-week-old ICR mice
  • Formulation: --
  • Dosages: 0.2 and 1 mg/kg
  • Administration: Oral treatment/subcutaneous administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (48.22 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 414.68
Formula

C16H17BrClN3O3

CAS No. 55837-20-2
Storage powder
in solvent
Synonyms N/A
Smiles OC1CCCNC1CC(=O)CN2C=NC3=CC(=C(Cl)C=C3C2=O)Br

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02630121 Recruiting Drug: Oxymetazoline Hydrochloride|Drug: Placebo Sleep Apnea|Chronic Nasal Congestion University of South Florida June 3 2019 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID