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Halofuginone
別名：RU-19110
Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
CAS No. 55837-20-2
文献中Selleckの製品使用例（11）
製品安全説明書
現在のバッチを見る：
S814401
DMSO]
8 mg/mL]
false]
Water]
Insoluble]
false]
Ethanol]
Insoluble]
false
純度：
99.81%
99.81
Halofuginone関連製品
シグナル伝達経路
DNA/RNA Synthesis阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| HuH7 | Antiplasmodial assay | 1 hr | Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay, IC50=0.017μM. | 23701465 | |
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal. | ||||
|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | 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]. | |||
|---|---|---|---|---|
| Kinase Assay | 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. | ||||
| 細胞実験 | 細胞株 | primary murine CD4+ CD25− T cells/MEFs | ||
| 濃度 | 5-20nM | |||
| 反応時間 | 4 or 24hrs | |||
| 実験の流れ | Primary murine CD4+ CD25− T cells are activated through the TCR in Th17 polarizing conditions in the presence of either 10nM 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). |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Growth inhibition assay | Cell viability |
|
22393274 | |
| Western blot | PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 p15 / p21 / E-cadherin / MMP2 / MMP9 / MMP14 / CD44 c-IAP / Mcl-1 p-JNK / JNK / p-p38 / p38 ATG7 |
|
26015407 | |
| In Vivo | ||
| In Vivo | 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]. | |
|---|---|---|
| 動物実験 | 動物モデル | 4- to 5-week-old ICR mice |
| 投与量 | 0.2 and 1 mg/kg | |
| 投与経路 | Oral treatment/subcutaneous administration | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04172779 | Not yet recruiting | Cirrhosis Liver |
University of Texas Southwestern Medical Center|National Cancer Institute (NCI) |
July 2024 | Phase 2 |
| NCT05279001 | Recruiting | Myelofibrosis |
Suzhou Zelgen Biopharmaceuticals Co.Ltd |
July 1 2024 | Phase 1 |
| NCT06316336 | Not yet recruiting | Healthy Vollunteer |
Pharma Nueva |
June 10 2024 | Phase 1 |
| NCT06156761 | Not yet recruiting | Breast Cancer |
Cancer Institute and Hospital Chinese Academy of Medical Sciences|CSPC Ouyi Pharmaceutical Co. Ltd. |
November 28 2023 | Not Applicable |
化学情報
| 分子量 | 414.68 | 化学式 | C16H17BrClN3O3 |
| CAS No. | 55837-20-2 | SDF | Download Halofuginone SDFをダウンロードする |
| Smiles | C1CC(C(NC1)CC(=O)CN2C=NC3=CC(=C(C=C3C2=O)Cl)Br)O | ||
| 保管 | |||
|
In vitro |
DMSO : 8 mg/mL ( (19.29 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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