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Halofuginone
$99 – $825
Products Details
Product 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].
Web ID
– HY-N1584
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– COVID-19-anti-virus
Molecular Formula
– C16H17BrClN3O3
Citations
– 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.|Hum Gene Ther. 2021 Aug 18.
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
– 55837-20-2
Molecular Weight
– 414.68
Compound Purity
– 99.78
SMILES
– O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3
Clinical Information
– Phase 2
Research Area
– Cancer; Infection; Inflammation/Immunology; Cardiovascular Disease
Solubility
– DMSO : 20 mg/mL (ultrasonic;adjust pH to 5 with HCl)
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
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