Halofuginone (hydrobromide)

Halofuginone (hydrobromide)

• CAS Number: 64924-67-0
• UNSPSC 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].
• Target Antigen: 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 Weight: 495.59
• 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.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.|Fish Shellfish Immunol. 2024 Jun 25:109727.|Friedrich-Alexander University Erlangen-Nuremberg. 2023 May 2.|Indian J Hematol Blood Transfus. 2024 Mar 25.|iScience. 2023 Mar.|J Funct Foods. 2024 Jul.|J Tissue Eng Regen Med. 2021 Aug 7.|Photodiagnosis Photodyn Ther. 2021 Oct 7;102572.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Phase 2