Halofuginone

SKU: orb1300403

Description

Halofuginone is a potent, competitive inhibitor of prolyl-tRNA synthetase (Ki=18.3 nM) that downregulates Smad3 and blocks TGF-β signaling at low nanomolar concentrations. This small molecule is a valuable research tool for studying fibrotic diseases, cancer biology, and T-cell differentiation in both cellular and animal models.

Research Area

Cell Biology, Infectious Disease & Virology, Metabolism Research, Molecular Biology, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 55837-20-2
• MW: 414.68
• Purity: 99.53%
• Formula: C₁₆H₁₇BrClN₃O₃
• SMILES: O[C@@H]1CCCN[C@H]1CC(=O)Cn1cnc2cc(Br)c(Cl)cc2c1=O
• Target: Sodium Channel,DNA/RNA Synthesis,Parasite,Calcium Channel,TGF-beta/Smad
• Solubility: DMSO:4.15 mg/mL (10.01 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.41 mM)

Bioactivity

• Target IC50:
  Prolyl-tRNA synthetase:18.3nM(Ki)
• 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.
• 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.
• Cell Research:
  Primary murine CD4+ CD25− T cells are activated through the TCR in Th17 polarizing conditions in the presence of either 10 nM 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNA Synthesis, DNA/RNA Synthesis, DNASynthesis, collagen, collagen-1, CalciumChannel, Calcium Channel, osteoarthritis, Parasite, Halofuginone, prolyl-tRNA, prolyl-tRNA synthetase, RU 19110, RU19110, RU-19110, RNASynthesis, RNA Synthesis, Sodium Channel, SodiumChannel, Smad, Tempostatin, TGFb, TGF-β, TGF-β/Smad, TGFbeta, TGF-b/Smad, TGF-beta, TGFbeta/Smad, TGF-beta/Smad, TGFβ, Transforming growth factor beta, type-I

Compound Identifiers

PubChem CID

400772