货号 | 13370-5mg |
描述 | Halofuginone is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.1 It has antimalarial and anticoccidial actions.1 In mammals, halofuginone at 10 ng/ml down-regulates Smad3, blocking TGF-β signaling and preventing both the differentiation of fibroblasts to myofibroblasts and the transitioning of epithelial cells to mesenchymal cells.1,2 Through this action, halofuginone blocks fibrosis and tumor progression in a variety of different models.1,3 This compound also competitively inhibits prolyl-tRNA synthetase (Ki = 18.3 nM), activating the amino acid starvation response.4,5 This prevents the differentiation of TH17 cells, blunting an autoimmune response.5 |
供应商 | Cayman |
应用文献 | |
1.McLaughlin, N.P.,Evans, P., and Pines, M. The chemistry and biology of febrifugine and halofuginone. Bioorganic & Medicinal Chemistry 22(7), 1993-2004 (2014). 2.Nelson, E.F.,Huang, C.W.,Ewel, J.M., et al. Halofuginone down-regulates Smad3 expression and inhibits the TGβinduced expression of fibrotic markers in human corneal fibroblasts. Molecular Vision 18, 479-487 (2012). 3.Pines, M.,Snyder, D.,Yarkoni, S., et al. Halofuginone to treat fibrosis in chronic graft-versus-host disease and scleroderma. Biology of Blood and Marrow Transplantation 9(7), 417-425 (2003). 4.Keller, T.L.,Zocco, D.,Sundrud, M.S., et al. Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nature Chemical Biology 8(3), 311-317 (2012). 5.Sundrud, M.S.,Koralov, S.B.,Feuerer, M., et al. Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response. Science 324, 1334-1338 (2009). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 451.1 |
分子式 | C16H17BrClN3O3 • HCl |
CAS号 | 1217623-74-9 |
稳定性 | ≥ 2 years |
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