Halofuginone lactate
Based on 22 publication(s) in Google Scholar
Halofuginone 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.
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- Reinheit: 98.32%
- CAS. Nr.: 82186-71-8
- Formel: C19H23BrClN3O6
- Molecular Weight:504.76
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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 Jun 25:109727. [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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Chemical Information
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CAS. Nr. 82186-71-8
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Appearance Solid
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Molecular Weight 504.76
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-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 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 -
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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Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (276 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)
Verweise
[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 |
Halofuginone lactate Related Classifications
HY-N1584C Related Classifications
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