Halofuginone

Catalog No.S8144 Synonyms: RU-19110

For research use only.

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

CAS No. 55837-20-2

Selleck's Halofuginone has been cited by 5 Publications

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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 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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HuH7 Mn\HRY51cXCuYYPtc4Rq[WxiYYPzZZk> NYO0W2hUOSCqch?= NE[5fHdCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTDh[4FqdnO2IHzpeoVzKHO2YXflJHBt[XOvb3TpeY0h[mW{Z3jlbUBqdm[nY4Tl[EBqdiCqdX3hckBJfUh5IHPlcIx{KGOxLXX4dJJme3OrbnegS2ZRNUy3Y3PvckB1emWjdHXkJIZweiBzIHjyJJBzcW:{IITvJIlv\mWldHnvckBnd2yub4fl[EBjgSB{NDDodpMh[W[2ZYKgZ49ueG:3bnSge4F{cG:3dDDt[YF{fXKnZDDh[pRmeiB2ODDodpMheG:|dD3pcoZm[3Srb36gZpkhSWyjbXHyJGJtfWViYYPzZZktKEmFNUC9NE4xOTgQvF2u NFX0fm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ewNVQ3PSd-MkO3NFE1PjV:L3G+
Assay
Methods Test Index 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 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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). 

Animal Research:

[4]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 414.68
Formula

C16H17BrClN3O3

CAS No. 55837-20-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(C(NC1)CC(=O)CN2C=NC3=CC(=C(C=C3C2=O)Cl)Br)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting Drug: Erlotinib Hydrochloride Cirrhosis Liver University of Texas Southwestern Medical Center July 2022 Phase 2
NCT05279001 Not yet recruiting Drug: Jaktinib Hydrochloride Tablet Myelofibrosis Suzhou Zelgen Biopharmaceuticals Co.Ltd May 1 2022 Phase 1
NCT05257018 Recruiting Drug: R-CDOP+intrathecal MTX Diffuse Large B-cell Lymphoma Fudan University February 26 2022 Phase 2
NCT02630121 Recruiting Drug: Oxymetazoline Hydrochloride|Drug: Placebo Sleep Apnea|Chronic Nasal Congestion University of South Florida January 2022 Phase 4
NCT05063851 Recruiting Drug: Memantine Hydrochloride Tablets|Drug: Placebo Alzheimer Disease University of Virginia October 11 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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