Halofuginone
Based on 22 publication(s) in Google Scholar
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
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- Pureté: 99.28%
- CAS No.: 55837-20-2
- Formule: C16H17BrClN3O3
- Masse moléculaire:414.68
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Halofuginone
More- Cell Metab. 2023 Dec 5;35(12):2216-2230.e8. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Aug 19;122(33):e2514837122. [Abstract]
- Phytomedicine. 2025 Jul 25:143:156788. [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]
- RNA. 2026 Feb 8:rna.080883.125. [Abstract]
- iScience. 2023 Mar 4;26(4):106334. [Abstract]
- Tissue Eng Regen Med. 2021 Dec;18(6):963-973. [Abstract]
- Antiviral Res. 2026 Jun:250:106417. [Abstract]
- J Funct Foods. 2024 Jul.
- Hum Gene Ther. 2022 Mar;33(5-6):237-249. [Abstract]
- Fish Shellfish Immunol. 2024 Jun 25:109727. [Abstract]
- J Virol. 2026 May 19;100(5):e0011726. [Abstract]
- ACS Infect Dis. 2023 Apr 14;9(4):1004-1021. [Abstract]
- 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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Activité biologique
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Plasmodium |
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Cell Line
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Type | Value | Description | References |
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| Huh-7 | IC50 |
0.017 μM
Compound: 2, HF
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Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay
Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay
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[PMID: 23701465] |
Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase[1].
The IC50s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC50s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively[1].
Halofuginone 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 (0.03-1μM) 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.
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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.
Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone[1].
Intraperitoneal administration of Halofuginone (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice[5].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 55837-20-2
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Appearance Solid
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Masse moléculaire 414.68
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Formule C16H17BrClN3O3
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Color White to off-white
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SMILES
O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3
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Synonyms
RU-19110
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 -
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 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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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 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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Br J Pharmacol
2025 Aug 13. PMID: 40803344 -
Br J Pharmacol
2021 Sep;178(17):3373-3394. PMID: 33694155
Halofuginone 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 -
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 -
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 -
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 -
Antiviral Res
Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]2026 Jun:250:106417. PMID: 42025967 -
Halofuginone 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 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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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 -
Fish Shellfish Immunol
Loss of Gcn2 exacerbates gossypol induced oxidative stress, apoptosis and inflammation in zebrafish. [Abstract]2024 Jun 25:109727. 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 -
ACS Infect Dis
2023 Apr 14;9(4):1004-1021. PMID: 36919909 -
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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Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Halofuginone Related Classifications
HY-N1584 Related Classifications
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