常山酮 T6856

Product Introduction
Bioactivity


英文名: Halofuginone

描述: Halofuginone (RU-19110) 是Febrifugine 的衍生物，是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂，可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。

细胞实验: Primary murine CD4+ CD25− T cells are activated through the TCR in Th17 polarizing conditions in the presence of either 10 nM MAZ1310 or HF and amino acid supplements. Th17 differentiation is assayed in the absence or presence of HF or borrelidin, with or without 1 mM threonine or proline supplementation. MEFs are treated with or without HF (50 nM) and/or Proline (2 mM) for 4 hours (CHOP, S100A4) or 24 hours (ColIA1, Col1A2).  (Only for Reference)

激酶实验: Assay of ProRS activity: The prolyl tRNA synthetase domain of human EPRS (ProRS) is expressed in E.coli with a 6-his tag and purified. Enzymatic activity is assayed using incorporation of 3H Pro into the tRNA fraction essentially, except that the charged tRNA fraction is isolated by rapid batchwise binding to Mono Q sepharose and quantitated by liquid scintillation counting. For all kinetic assays, the concentration of active enzyme in the reaction is 40 nM. Similar inhibition by HF is seen using the human ProRS domain purified from bacteria and full length EPRS purified from rat liver.

体外活性: 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[2].

体内活性: Halofuginone clearly extends the survival times of the parasite-infected mice. Oral treatment with halofuginone at doses of 0.2 and 1 mg/kg has an apparent curative effect for the infected mice. The subcutaneous administration of 0.2 mg of halofuginone per kg likewise extends the survival times of the infected mice, but none of the mice is cured. The mice in the 5-mg/kg dose groups die before the completion of treatment with the drug either orally or subcutaneously. Subcutaneous treatment with halofuginone appears to be more toxic to mice than oral treatment[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16 mg/mL (38.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: osteoarthritis | collagen-1 | Na+ channels | Calcium Channel | Na channels | Transforming growth factor beta | prolyl-tRNA | TGF-beta/Smad | DNA/RNA Synthesis | Ca2+ channels | TGF-β | type-I | Ca channels | Sodium Channel | Parasite | inhibit | Halofuginone | collagen | RU19110 | Inhibitor | RU 19110

相关产品: 8(14),15-Isopimaradien-3-ol | Aranidipine | Semotiadil recemate fumarate | Teludipine hydrochloride | Calciseptin | TTA-A8 | PD0176078 | PD173212 | 1-(aminomethyl)cyclopropanecarboxylic acid hydrochloride | Cinepazide maleate

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Parasitic Compound Library | Anti-Pancreatic Cancer Compound Library | Antiparasitic Natural Product Library | TGF-beta/Smad Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途