Halofuginone, also known as RU-19110, is a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters.
Chemical Formula: C16H17BrClN3O3
Exact Mass: 413.01418
Molecular Weight: 414.68
Elemental Analysis: C, 46.34; H, 4.13; Br, 19.27; Cl, 8.55; N, 10.13; O, 11.57
Chemical Name: 7-bromo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one.
InChi Code: InChI=1S/C16H17BrClN3O3/c17-11-6-13-10(5-12(11)18)16(24)21(8-20-13)7-9(22)4-14-15(23)2-1-3-19-14/h5-6,8,14-15,19,23H,1-4,7H2/t14-,15+/m0/s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.
The IC50s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC50s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.
Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage.
Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone
- Pines M, Spector I. Halofuginone - The Multifaceted Molecule. Molecules. 2015 Jan 5;20(1):573-594. Review. PubMed PMID: 25569515.
- Pines M. Halofuginone for fibrosis, regeneration and cancer in the gastrointestinal tract. World J Gastroenterol. 2014 Oct 28;20(40):14778-86. doi: 10.3748/wjg.v20.i40.14778. PubMed PMID: 25356039; PubMed Central PMCID: PMC4209542.
- Guo LW, Wang B, Goel SA, Little C, Takayama T, Shi XD, Roenneburg D, DiRenzo D, Kent KC. Halofuginone stimulates adaptive remodeling and preserves re-endothelialization in balloon-injured rat carotid arteries. Circ Cardiovasc Interv. 2014 Aug;7(4):594-601. doi: 10.1161/CIRCINTERVENTIONS.113.001181. Epub 2014 Jul 29. PubMed PMID: 25074254; PubMed Central PMCID: PMC4140988.
- Park MK, Park JS, Park EM, Lim MA, Kim SM, Lee DG, Baek SY, Yang EJ, Woo JW, Lee J, Kwok SK, Kim HY, Cho ML, Park SH. Halofuginone ameliorates autoimmune arthritis in mice by regulating the balance between Th17 and Treg cells and inhibiting osteoclastogenesis. Arthritis Rheumatol. 2014 May;66(5):1195-207. doi: 10.1002/art.38313. PubMed PMID: 24782183.
- Bodanovsky A, Guttman N, Barzilai-Tutsch H, Genin O, Levy O, Pines M, Halevy O. Halofuginone improves muscle-cell survival in muscular dystrophies. Biochim Biophys Acta. 2014 Jul;1843(7):1339-47. doi: 10.1016/j.bbamcr.2014.03.025. Epub 2014 Apr 2. PubMed PMID: 24703880.
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