Halofuginone (lactate)

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

Product Specifications

CAS Number

[82186-71-8]

Product Name Alternative

RU-19110 (lactate)

UNSPSC

12352005

Hazard Statement

H301, H310, H315, H318, H330

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

Field of Research

Cancer; Infection; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/halofuginone-lactate.html

Concentration

10mM

Purity

98.32

Solubility

DMSO : 35 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C19H23BrClN3O6

Molecular Weight

504.76

Precautions

H301, H310, H315, H318, 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.