Halofuginone

Catalog No.S8144 Batch:S814401

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Technical Data

Formula

C16H17BrClN3O3
Molecular Weight 414.68 CAS No. 55837-20-2
Solubility (25°C)* In vitro DMSO 8 mg/mL (19.29 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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].
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 Assay:

[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 Study:

[4]
  • Animal Models

    4- to 5-week-old ICR mice

  • Dosages

    0.2 and 1 mg/kg

  • Administration

    Oral treatment/subcutaneous administration

Selleck's Halofuginone has been cited by 11 publications

Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
Dual effects of TGF-β inhibitor in ALS - inhibit contracture and neurodegeneration [ J Neurochem, 2024, 10.1111/jnc.16102] PubMed: 38515326
EPRS1 correlates with malignant progression in hepatocellular carcinoma [ Infect Agent Cancer, 2023, 18(1):27] PubMed: 37138286
Transforming growth factor-β receptor type 2 is required for heparin-binding protein-induced acute lung injury and vascular leakage for transforming growth factor-β/Smad/Rho signaling pathway activation [ FASEB J, 2022, 36(11):e22580] PubMed: 36189652
Integrated Stress Response Regulation of Corneal Epithelial Cell Motility and Cytokine Production [ Invest Ophthalmol Vis Sci, 2022, 63(8):1] PubMed: 35802384
A high-throughput screen for TMPRSS2 expression identifies FDA-approved compounds that can limit SARS-CoV-2 entry [ Nat Commun, 2021, 12(1):3907] PubMed: 34162861
Cancer-associated fibroblasts-derived HAPLN1 promotes tumour invasion through extracellular matrix remodeling in gastric cancer [ Gastric Cancer, 2021, 10.1007/s10120-021-01259-5] PubMed: 34724589
SARS-CoV-2 spike protein 13-mer subdomain corresponds to the drug-binding domain of glutamyl-propyl-tRNA synthetase 1 and is targetable by halofuginone [ Research Square, 2021, 10.21203/rs.3.rs-738132/v1] PubMed: None
Red-COLA1: a human fibroblast reporter cell line for type I collagen transcription [ Sci Rep, 2020, 10(1):19723] PubMed: 33184327
Halofuginone inhibits tumorigenic progression of 5-FU-resistant human colorectal cancer HCT-15/FU cells by targeting miR-132-3p in vitro [ Oncol Lett, 2020, 20(6):385] PubMed: 33154782

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.