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Halofuginone

CAT: 0804-HY-N1584-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-N1584-01Size:5 mg
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Description
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM[1][2]. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3][4]. 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[5].
CAS Number
[55837-20-2]
Product Name Alternative
RU-19110
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Calcium Channel; DNA/RNA Synthesis; Parasite; Sodium Channel; TGF-beta/Smad
Type
Natural Products
Related Pathways
Anti-infection; Cell Cycle/DNA Damage; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt; TGF-beta/Smad
Applications
COVID-19-anti-virus
Field of Research
Cancer; Infection; Inflammation/Immunology; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/Halofuginone.html
Purity
99.28
Solubility
DMSO : 20 mg/mL (ultrasonic; adjust pH to 5 with HCl)
Smiles
O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3
Molecular Formula
C16H17BrClN3O3
Molecular Weight
414.68
Precautions
H302, H315, H319, H335
References & Citations
[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.|[2]Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8 (3) :311-7.|[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.|[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.|[5]Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Natural Products
Clinical Information
Phase 2
Isoform
Plasmodium
Citation 01
ACS Infect Dis. 2023 Apr 14;9 (4) :1004-1021.|Anal Chem. 2025 Jun 3;97 (21) :11099-11109.|bioRxiv. 2025 April 12.|bioRxiv. 2025 July 11.|Br J Pharmacol. 2021 Sep;178 (17) :3373-3394.|Br J Pharmacol. 2025 Aug 13.|Cell Metab. 2023 Dec 5;35 (12) :2216-2230.e8.|Fish Shellfish Immunol. 2024 Jun 25:109727.|Friedrich-Alexander University Erlangen-Nuremberg. 2023 May 2.|Indian J Hematol Blood Transfus. 2024 Jul;40 (3) :407-414.|iScience. 2023 Mar 4;26 (4) :106334.|J Funct Foods. 2024 Jul.|Photodiagnosis Photodyn Ther. 2022 Mar:37:102572.|Phytomedicine. 2025 Jul 25:143:156788.|Proc Natl Acad Sci U S A. 2025 Aug 19;122 (33) :e2514837122.|Rutgers University. 2025.|Tissue Eng Regen Med. 2021 Dec;18 (6) :963-973.|Hum Gene Ther. 2022 Mar;33 (5-6) :237-249.

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