Products Details

Product 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].

Web ID

– HY-N1584A

Storage Temperature

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

Shipping

– Room Temperature

Applications

– COVID-19-anti-virus

Molecular Formula

– C16H18Br2ClN3O3

Citations

– Hum Gene Ther. 2021 Aug 18.|ACS Infect Dis. 2023 Mar 15.|Br J Pharmacol. 2021 Mar 10.|Cell Metab. 2023 Nov 11:S1550-4131(23)00385-6.|Friedrich-Alexander University Erlangen-Nuremberg. 2023 May 2.|iScience. 2023 Mar.|J Tissue Eng Regen Med. 2021 Aug 7.|Photodiagnosis Photodyn Ther. 2021 Oct 7;102572.

References

– [1]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.|[2]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.|[3]Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7.|[4]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.|[5]Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10.

CAS Number

– 64924-67-0

Molecular Weight

– 495.59

Compound Purity

– 99.99

SMILES

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

Clinical Information

– Phase 2

Research Area

– Cancer; Infection; Inflammation/Immunology; Cardiovascular Disease

Solubility

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

Target

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

Isoform

– Plasmodium

Pathway

– Anti-infection;Cell Cycle/DNA Damage;Membrane Transporter/Ion Channel;Neuronal Signaling;Stem Cell/Wnt;TGF-beta/Smad

Product type

– Natural Products

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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