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Halofuginone

Catalog No. T6856 CAS 55837-20-2

Synonyms: Tempostatin, empostatin, RU-19110

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

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Halofuginone, CAS 55837-20-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 79.00
10 mg	In stock	$ 125.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 382.00
100 mg	In stock	$ 575.00
500 mg	In stock	$ 1,260.00
1 mL * 10 mM (in DMSO)	In stock	$ 88.00

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Purity: 97.67%

Purity: 95.35%

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Storage & Solubility Information

Description	Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in the mammal.
Targets&IC50	Prolyl-tRNA synthetase: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].
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	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)
Source	Natural Products > Saxifragaceae > Dichroa

Synonyms	Tempostatin, empostatin, RU-19110
Molecular Weight	414.68
Formula	C16H17BrClN3O3
CAS No.	55837-20-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 16 mg/mL (38.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Keller TL, et al. Nat Chem Biol. 2012, 8(3):311-317. 2. Nelson EF, et al. Molecular Vision. 2012, 18:479-487. 3. McLaughlin NP, et al. Bioorg Med Chem. 2014, 22(7):11993-22004. 4. Jiang S, et al. Antimicrob Agents Chemother. 2005, 49(3):1169-1176. 6. Tsuchida K, et al. Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Free Radic Biol Med. 2017 Feb;103:236-247.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library TGF-beta/Smad Compound Library Anti-Parasitic Compound Library Antiparasitic Natural Product Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compounds Library Max

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Keywords

Halofuginone 55837-20-2 Cell Cycle/Checkpoint DNA Damage/DNA Repair Membrane transporter/Ion channel Metabolism Microbiology/Virology Stem Cells DNA/RNA Synthesis Sodium Channel Calcium Channel Parasite TGF-beta/Smad osteoarthritis collagen-1 Na+ channels Na channels Transforming growth factor beta prolyl-tRNA Ca2+ channels TGF-β type-I Ca channels inhibit collagen Tempostatin RU19110 empostatin Inhibitor RU 19110 RU-19110 inhibitor

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