Halofuginone (hydrobromide)

• Description:

  Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM[1][2]. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3][4]. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects[5].

• Product Name Alternative:

  RU-19110 (hydrobromide)

• UNSPSC:

  12352005

• Hazard Statement:

  H300+H310+H330

• 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_hydrobromide.html

• Purity:

  99.99

• Solubility:

  DMSO : 50 mg/mL (ultrasonic) |H2O : 2.6 mg/mL (ultrasonic)

• Smiles:

  O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3.Br

• Molecular Formula:

  C16H18Br2ClN3O3

• Molecular Weight:

  495.59

• Precautions:

  H300+H310+H330

• 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:

  4°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Natural Products

• Clinical Information:

  Phase 2

• Isoform:

  Plasmodium

• Citation 01:

  Hum Gene Ther. 2022 Mar;33 (5-6) :237-249.|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.

• CAS Number:

  [64924-67-0]