Halofuginone (hydrochloride)

Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. 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[1][2][3][4][5].

Product Specifications

CAS Number

[1217623-74-9]

Product Name Alternative

RU-19110 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302

Target

Calcium Channel; DNA/RNA Synthesis; Parasite; Sodium Channel; TGF-beta/Smad

Type

Reference compound

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-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C1C2=CC(Cl)=C(Br)C=C2N=CN1CC(C[C@H]3[C@@H](CCCN3)O)=O.Cl

Molecular Formula

C16H18BrCl2N3O3

Molecular Weight

451.14

Precautions

P264-P270-P330-P501

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.