Halofuginone lactate
Based on 22 publication(s) in Google Scholar
Halofuginone lactate (RU-19110 lactate), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
For research use only. We do not sell to patients.
- Purity : 98.32%
- CAS No.: 82186-71-8
- Formula: C19H23BrClN3O6
- Molecular Weight:504.76
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Halofuginone lactate
More- Cell Metab. 2023 Dec 5;35(12):2216-2230.e8. [Abstract]
- Phytomedicine. 2025 Jul 25:143:156788. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Aug 19;122(33):e2514837122. [Abstract]
- Br J Pharmacol. 2025 Aug 13. [Abstract]
- Br J Pharmacol. 2021 Sep;178(17):3373-3394. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Tissue Eng Regen Med. 2021 Dec;18(6):963-973. [Abstract]
- Hum Gene Ther. 2022 Mar;33(5-6):237-249. [Abstract]
- ACS Infect Dis. 2023 Apr 14;9(4):1004-1021. [Abstract]
- iScience. 2023 Mar 4;26(4):106334. [Abstract]
- Antiviral Res. 2026 Jun:250:106417. [Abstract]
- RNA. 2026 Feb 8:rna.080883.125. [Abstract]
- Fish Shellfish Immunol. 2024 Aug:151:109727. [Abstract]
- J Virol. 2026 May 19;100(5):e0011726. [Abstract]
- J Funct Foods. 2024 Jul.
- Photodiagnosis Photodyn Ther. 2022 Mar:37:102572. [Abstract]
- Indian J Hematol Blood Transfus. 2024 Jul;40(3):407-414. [Abstract]
- bioRxiv. 2026 Jan 15.
- bioRxiv. 2025 July 11.
- Rutgers University. 2025.
- bioRxiv. 2025 April 12.
- Friedrich-Alexander University Erlangen-Nuremberg. 2023 May 2.
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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WB
All DNA/RNA Synthesis Isoforms
MoreAll Parasite Isoforms
MoreAll Calcium Channel Isoforms
More
Biological Activity
Description
IC50 & Target
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Plasmodium |
In Vitro
Halofuginone lactate competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase[1].
The IC50s of Halofuginone lactate (1-10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC50s of Halofuginone lactate (1-1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC50 of Halofuginone lactate for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively[1].
Halofuginone lactate increases voltage-gated K+ (Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K+ currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone lactate inhibits receptor-operated Ca2+ entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuates store-operated Ca2+ entry (SOCE) in PASMC[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation
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Concentration:1, 10, 100, 1000, 10000 nM
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Incubation Time:48 hours
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Result:The IC50s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
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Cell Line:KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation.
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:24 hours
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Result:The IC50s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:3-month-old male C57BL/6J (WT) mice[3]
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Dosage:0.2, 0.5, 1 or 2.5 mg/kg
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Administration:Injected intraperitoneally every other day for 1 month
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Result:Attenuated progression of OA in ACLT mice.
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Animal Model:Male nude mice (BALB/C nu/nu mice) (6-8-week)[1]
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Dosage:0.25 mg/kg
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Administration:Intraperitoneally injected; every day; 16 days
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Result:The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased.
Chemical Information
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CAS No. 82186-71-8
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Appearance Solid
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Molecular Weight 504.76
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Formula C19H23BrClN3O6
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Color White to off-white
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SMILES
OC(C(O)C)=O.O=C1C2=CC(Cl)=C(Br)C=C2N=CN1CC(C[C@H]3[C@@H](CCCN3)O)=O
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Synonyms
RU-19110 lactate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (22)
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Journal Impact Factor
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Most Recent
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Cell Metab
2023 Dec 5;35(12):2216-2230.e8. PMID: 37979583 -
Phytomedicine
Halofuginone targets Serine/Glycine synthesis to reverse epidermal growth factor receptor Tyrosine Kinase inhibitor resistance in lung adenocarcinoma. [Abstract]2025 Jul 25:143:156788. PMID: 40354707
Halofuginone lactate purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Jul 25:143:156788. [Abstract]
Cell morphology under the microscope after 24 h of 4 μM AUM in combination with 50 nM Halofuginone (HF) in the resistant cell lines and inhibition of colony formation.
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Proc Natl Acad Sci U S A
Stress granule-mediated ZBP1 activation drives necroptotic cell death in non-obstructive azoospermia and testicular aging. [Abstract]2025 Aug 19;122(33):e2514837122. PMID: 40811463
Halofuginone lactate purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Aug 19;122(33):e2514837122. [Abstract]
Cultured L929, L929(Pkr-/-Hri-/-Perk-/-Gcn2-/-), L929(G3bp1-/-G3bp2-/-), L929(Zbp1-/-), L929(Ripk3-/-) and L929(Mlkl-/-) cells were treated Halofuginone (500 nM) and Halofuginone (500 nM)+IFN-β(10 ng/ml) for 42 hours; The intracellular ATP levels were measured by Cell Titer-Glo.
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Br J Pharmacol
2025 Aug 13. PMID: 40803344 -
Br J Pharmacol
2021 Sep;178(17):3373-3394. PMID: 33694155
Halofuginone lactate purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Sep;178(17):3373-3394. [Abstract]
Western blot analysis on p-Akt, Akt, p-mTOR and mTOR in control PASMCs and PASMCs treated with PDGF in the absence (vehicle control, Veh) and presence (Halofuginone; HF) of 1 μM halofuginone (for 24 h).
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Tissue Eng Regen Med
Three-Dimensional Modeling of the Structural Microenvironment in Post-Traumatic War Wounds. [Abstract]2021 Dec;18(6):963-973. PMID: 34363599 -
Hum Gene Ther
Antifibrotic Therapy Augments the Antitumor Effects of Vesicular Stomatitis Virus Via Reprogramming Tumor Microenvironment. [Abstract]2022 Mar;33(5-6):237-249. PMID: 34405694 -
ACS Infect Dis
2023 Apr 14;9(4):1004-1021. PMID: 36919909 -
iScience
EtcPRS Mut as a molecular marker of halofuginone resistance in Eimeria tenella and Toxoplasma gondii. [Abstract]2023 Mar 4;26(4):106334. PMID: 36968087 -
Antiviral Res
Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]2026 Jun:250:106417. PMID: 42025967 -
RNA
Tuning tRNA synthetase inhibition reveals parabolic induction of stress granules limited in size and RNA content. [Abstract]2026 Feb 8:rna.080883.125. PMID: 41656003 -
Fish Shellfish Immunol
Loss of Gcn2 exacerbates gossypol induced oxidative stress, apoptosis and inflammation in zebrafish. [Abstract]2024 Aug:151:109727. PMID: 38936520 -
J Virol
Febrifugine dihydrochloride restricts porcine epidemic diarrhea virus replication by modulating the IGF1R-driven PI3K/AKT-apoptosis axis. [Abstract]2026 May 19;100(5):e0011726. PMID: 41983768 -
Halofuginone lactate purchased from MedChemExpress. Usage Cited in: J Funct Foods. 2024 Jul.
Cell viability measured by MTT assay after treatment with 100, 200, 400, 800, and 1000 nM concentrations of Halofuginone (HF) in parental cells MDA-MB-231 and BT-20 for 24 h, as well as resistant cells MDA-MB-231/PR and BT-20/PR.
Halofuginone lactate purchased from MedChemExpress. Usage Cited in: J Funct Foods. 2024 Jul.
Halofuginone (HF; 200 nM; 24 h) treated MDA-MB-231/PR and BT20/PR cells reduced cell invasion capabilities.
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Photodiagnosis Photodyn Ther
Halofuginone enhances the anti-tumor effect of ALA-PDT by suppressing NRF2 signaling in cSCC. [Abstract]2022 Mar:37:102572. PMID: 34628069 -
Indian J Hematol Blood Transfus
Halofuginone Inhibits Osteoclastogenesis and Enhances Osteoblastogenesis by Regulating Th17/Treg Cell Balance in Multiple Myeloma Mice with Bone Lesions. [Abstract]2024 Jul;40(3):407-414. PMID: 39011260 -
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Solvent & Solubility
In Vitro:
DMSO : 35 mg/mL (69.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (293 KB)
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SDS (642 KB)
- English - EN (642 KB)
- Français - FR (642 KB)
- Deutsch - DE (642 KB)
- Norwegian - NO (642 KB)
- Español - ES (642 KB)
- Swedish - SV (642 KB)
- Italian - IT (642 KB)
- Korean - KR (642 KB)
- Portuguese - PT (642 KB)
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Handling Instructions (2659 KB)
References
[1]. 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. [Content Brief]
[2]. Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7. [Content Brief]
[3]. Cui Z, et al. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone. Ann Rheum Dis. 2016 Sep;75(9):1714-21. [Content Brief]
[4]. Tracy L McGaha, et al. Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts. J Invest Dermatol. 2002 Mar;118(3):461-70. [Content Brief]
[5]. Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9811 mL | 9.9057 mL | 19.8114 mL | 49.5285 mL |
| 5 mM | 0.3962 mL | 1.9811 mL | 3.9623 mL | 9.9057 mL | |
| 10 mM | 0.1981 mL | 0.9906 mL | 1.9811 mL | 4.9528 mL | |
| 15 mM | 0.1321 mL | 0.6604 mL | 1.3208 mL | 3.3019 mL | |
| 20 mM | 0.0991 mL | 0.4953 mL | 0.9906 mL | 2.4764 mL | |
| 25 mM | 0.0792 mL | 0.3962 mL | 0.7925 mL | 1.9811 mL | |
| 30 mM | 0.0660 mL | 0.3302 mL | 0.6604 mL | 1.6509 mL | |
| 40 mM | 0.0495 mL | 0.2476 mL | 0.4953 mL | 1.2382 mL | |
| 50 mM | 0.0396 mL | 0.1981 mL | 0.3962 mL | 0.9906 mL | |
| 60 mM | 0.0330 mL | 0.1651 mL | 0.3302 mL | 0.8255 mL |