Halofuginone hydrobromide

Halofuginone hydrobromid 是Febrifugine 的衍生物,是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂,并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。

CAS号

64924-67-0

分子式

C16H17BrClN3O3.HBr

主要靶点

Others|Sodium Channel|Calcium Channel|TGF-beta/Smad|Parasite|DNA/RNA Synthesis

仅限科研使用

Cat No : CM05547

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Synonyms

常山酮溴酸盐|Stenorol|卤夫酮溴氢酸盐|Tempostatin|RU-19110 (hydrobromide)



产品信息

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. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

CAS号 64924-67-0
分子式 C16H17BrClN3O3.HBr
主要靶点 Others|Sodium Channel|Calcium Channel|TGF-beta/Smad|Parasite|DNA/RNA Synthesis
主要通路 其他|干细胞|DNA损伤和修复|细胞周期|离子通道|微生物学|代谢
分子量 495.59
纯度 98.50%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 常山酮溴酸盐|Stenorol|卤夫酮溴氢酸盐|Tempostatin|RU-19110 (hydrobromide)

靶点活性

prolyl-tRNA synthetase:18.3±0.5 nM(ki)

溶解度

DMSO:49.6 mg/mL (100 mM)

参考文献

1.Zhou H. et al. ATP-directed capture of bioactive herbal-based medicine on human tRNA synthetase. Nature. 2013 Feb 7;494(7435):121-4.
2.Keller TL., et al. Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7.

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