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Halofuginone CAS: 55837-20-2

Category: Inhibitors
Product Name: Halofuginone
Cat No: I000014
CAS No: 55837-20-2
Synonyms: RU 19110; RU19110; RU-19110; Halofuginone; Tempostatin.
Molecular Formula: C16H17BrClN3O3
Molecular Weight: 414.68
SMILES: O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3
InChI: None
InChIKey: None
Solubility: DMSO: ≥ 9 mg/mL
Target: None
CAS 55837-20-2,Halofuginone
  • Description

Halofuginone(cas 55837-20-2) inhibits the development of T helper 17 cells, immune cells that play an important role in autoimmune disease, but it does not affect other kinds of T cells which are involved in normal immune function. Halofuginone therefore has potential for the treatment of autoimmune disorders.
Halofuginone is also an inhibitor of collagen type I gene expression and as a consequence it may inhibit tumor cell growth. Halofuginone exerts its effects by acting as a high affinity inhibitor of the enzyme glutamyl-prolyl tRNA synthetase. Inhibition of prolyl tRNA charging leads to the accumulation of uncharged prolyl tRNAs, which serve as a signal to initiate the amino acid starvation response, which in turn exerts anti-inflammatory and anti-fibrotic effects. (source: https://en.wikipedia.org/wiki/Halofuginone).
In vitro: The addition of halofuginone can significantly inhibit the migratory and invasive trend induced by irradiation, and the TGF-β pathway was also inhibited. In the study, we observed the strong inhibitory activity of halofuginone on HepG2 cell growth and the cell cycle and apoptosis assays showed that halofuginone arrested the cell cycle and inhibited the induction. And we found that halofuginone inhibits tumor cell cycle possibly by up-regulating p15 and p21 of expression. Then, we found that the proportion of cleaved PARP, caspase-3, 8 and 9 in HepG2 cells increased after halofuginone treatment. And the results showed that halofuginone down-regulated Mcl-1 and c-IAP1 expression. Finally, our results showed halofuginone regulated the activities of JNK and MEK/ERK signaling pathways in hepatocellular carcinoma cells.
In vivo: In animal xenograft model, the addition of halofuginone to irradiation inhibited the growth of subcutaneously implanted xenografts, reduced hepatic and pulmonary metastases, and improved survival of the mice. C57BL/6 recipient mice received an orthotopic left lung transplant, and Lung transplant recipients received daily intraperitoneal injections of 2.5 μg halofuginone or vehicle alone. Lung grafts were assessed on Days 7, 14, and 28 post-transplant. Compared with control mice, on Day 28 post-transplant, lung grafts of mice treated with halofuginone showed a significant reduction in the percentage of obliterated airways (6.8 ± 4.7% vs 52.5 ± 13.8%, p < 0.01), as well as significantly reduced parenchymal fibrosis (5.5 ± 2.3% vs 35.9 ± 10.9%, p < 0.05).

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:Halofuginone dually regulates autophagic flux through nutrient-sensing pathways in colorectal cancer. Chen GQ, Gong RH, Yang DJ, Zhang G, Lu AP, Yan SC, Lin SH, Bian ZX.Cell Death Dis. 2017 May 11;8(5):e2789. doi: 10.1038/cddis.2017.203. PMID: 28492544
2:Effect of Halofuginone on the Pathogenesis of Autoimmune Thyroid Disease in Different Mice Models. Hou X, Zhou J, Yang R, Liu S, Bi M, Liu T, Fan C, Guan H, Li Y, Shan Z, Teng W.Endocr Metab Immune Disord Drug Targets. 2017 Apr 23. doi: 10.2174/1871530317666170424101256. [Epub ahead of print] PMID: 28440200
3:Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Tsuchida K, Tsujita T, Hayashi M, Ojima A, Keleku-Lukwete N, Katsuoka F, Otsuki A, Kikuchi H, Oshima Y, Suzuki M, Yamamoto M.Free Radic Biol Med. 2017 Feb;103:236-247. doi: 10.1016/j.freeradbiomed.2016.12.041. Epub 2016 Dec 28. PMID: 28039084
4:Halofuginone inhibits TNF-α-induced the migration and proliferation of fibroblast-like synoviocytes from rheumatoid arthritis patients. Zeng S, Wang K, Huang M, Qiu Q, Xiao Y, Shi M, Zou Y, Yang X, Xu H, Liang L.Int Immunopharmacol. 2017 Feb;43:187-194. doi: 10.1016/j.intimp.2016.12.016. Epub 2016 Dec 23. PMID: 28013187
5:Halofuginone inhibits radiotherapy-induced epithelial-mesenchymal transition in lung cancer. Chen Y, Liu W, Wang P, Hou H, Liu N, Gong L, Wang Y, Ji K, Zhao L, Wang P.Oncotarget. 2016 Nov 1;7(44):71341-71352. doi: 10.18632/oncotarget.11217. PMID: 27533085 Free PMC Article
6:Amelioration of radiation-induced lung injury by halofuginone: An experimental study in Wistar-Albino rats. Calik M, Yavas G, Calik SG, Yavas C, Celik ZE, Sargon MF, Esme H.Hum Exp Toxicol. 2016 Jul 24. pii: 0960327116660753. [Epub ahead of print] PMID: 27457799
7:Halofuginone Alleviates Burn-Induced Hepatic and Renal Damage in Rats. Cerit KK, Karakoyun B, Yüksel M, Ercan F, Tuğtepe H, Dagli TE, Yeğen BÇ.J Burn Care Res. 2017 Jan/Feb;38(1):e384-e394. doi: 10.1097/BCR.0000000000000400. PMID: 27388880
8:Halofuginone and artemisinin synergistically arrest cancer cells at the G1/G0 phase by upregulating p21Cip1 and p27Kip1. Chen G, Gong R, Shi X, Yang D, Zhang G, Lu A, Yue J, Bian Z.Oncotarget. 2016 Aug 2;7(31):50302-50314. doi: 10.18632/oncotarget.10367. PMID: 27385212 Free PMC Article
9:Halofuginone reduces the inflammatory responses of DSS-induced colitis through metabolic reprogramming. Liu J, Xiao HT, Wang HS, Mu HX, Zhao L, Du J, Yang D, Wang D, Bian ZX, Lin SH.Mol Biosyst. 2016 Jun 21;12(7):2296-303. doi: 10.1039/c6mb00154h. PMID: 27197570
10:Halofuginone suppresses growth of human uterine leiomyoma cells in a mouse xenograft model. Koohestani F, Qiang W, MacNeill AL, Druschitz SA, Serna VA, Adur M, Kurita T, Nowak RA.Hum Reprod. 2016 Jul;31(7):1540-51. doi: 10.1093/humrep/dew094. Epub 2016 Apr 29. PMID: 27130615


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