製品番号: HY-N1584B

Halofuginone hydrochloride

(別名: RU-19110 hydrochloride)

20 Cited Publications

カスタマーレビュー

Based on 20 publication(s) in Google Scholar

Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1217623-74-9
分子式: C₁₆H₁₈BrCl₂N₃O₃
分子量:451.14

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

Halofuginone hydrochloride 構造式

CAS 番号: 1217623-74-9

容量

価格（税別）

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数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (20)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)^[2]

Calcium Channel アイソフォーム固有の製品をすべて表示 :

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示 :

Parasite アイソフォーム固有の製品をすべて表示 :

Sodium Channel アイソフォーム固有の製品をすべて表示 :

TGF-beta/Smad アイソフォーム固有の製品をすべて表示 :

Smad1
Smad3

体外実験

Halofuginone hydrobromid competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase^[1].
The IC₅₀s of Halofuginone hydrobromid (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively^[1].
The IC₅₀s of Halofuginone hydrobromid (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC₅₀ of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively^[1].
Halofuginone hydrobromid increases voltage-gated K⁺ (Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K⁺ currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone (0.03-1μM) hydrobromid inhibits receptor-operated Ca²⁺ entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuated store-operated (SOCE) Ca²⁺ entry in PASMC^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation.
Concentration:

1, 10, 100, 1000, 10000 nM
Incubation Time:

24 h
Result:

The IC₅₀s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.

Cell Viability Assay^[1]

Cell Line:

KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation
Concentration:

1, 10, 100, 1000, 10000 nM
Incubation Time:

48 h
Result:

The IC₅₀s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.

体内実験

Halofuginone hydrobromid (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage^[3].
Halofuginone hydrobromid (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone hydrobromid (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone^[1].
Intraperitoneal hydrobromid administration of Halofuginone (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

3-month-old male C57BL/6J (WT) mice^[3]
Dosage:

0.2, 0.5, 1 or 2.5 mg/kg
Administration:

Injected intraperitoneally every other day for 1 month
Result:

Attenuated progression of OA in ACLT mice.

Animal Model:

Male nude mice (BALB/C nu/nu mice) (6-8-week)^[1]
Dosage:

0.25 mg/kg
Administration:

Intraperitoneally injected; every day; 16 days
Result:

The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased.

化学情報

CAS 番号 1217623-74-9
分子量 451.14
分子式 C₁₆H₁₈BrCl₂N₃O₃
SMILES

O=C1C2=CC(Cl)=C(Br)C=C2N=CN1CC(C[C@H]3[C@@H](CCCN3)O)=O.Cl
別名

RU-19110 hydrochloride
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (20)

All Bio/Physico-chemical AssayCell Imaging/StainingWBCell Proliferation/Viability AssayCell Migration/Invasion Assay

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Journal Impact Factor

Cell Metab

The tRNA-GCN2-FBXO22-axis-mediated mTOR ubiquitination senses amino acid insufficiency. [Abstract]

2023 Dec 5;35(12):2216-2230.e8. PMID: 37979583
Phytomedicine

Halofuginone targets Serine/Glycine synthesis to reverse epidermal growth factor receptor Tyrosine Kinase inhibitor resistance in lung adenocarcinoma. [Abstract]

2025 Jul 25:143:156788. PMID: 40354707

Halofuginone hydrochloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Jul 25:143:156788. [Abstract]

Cell morphology under the microscope after 24 h of 4 μM AUM in combination with 50 nM Halofuginone (HF) in the resistant cell lines and inhibition of colony formation.
Proc Natl Acad Sci U S A

Stress granule-mediated ZBP1 activation drives necroptotic cell death in non-obstructive azoospermia and testicular aging. [Abstract]

2025 Aug 19;122(33):e2514837122. PMID: 40811463

Halofuginone hydrochloride purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2025 Aug 19;122(33):e2514837122. [Abstract]

Cultured L929, L929(Pkr^-/-Hri^-/-Perk^-/-Gcn2^-/-), L929(G3bp1^-/-G3bp2^-/-), L929(Zbp1^-/-), L929(Ripk3^-/-) and L929(Mlkl^-/-) cells were treated Halofuginone (500 nM) and Halofuginone (500 nM)+IFN-β(10 ng/ml) for 42 hours; The intracellular ATP levels were measured by Cell Titer-Glo.
Br J Pharmacol

GCN2 regulates paclitaxel-induced neuropathic pain. [Abstract]

2025 Aug 13. PMID: 40803344
Br J Pharmacol

Halofuginone, a promising drug for treatment of pulmonary hypertension. [Abstract]

2021 Sep;178(17):3373-3394. PMID: 33694155

Halofuginone hydrochloride purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2021 Sep;178(17):3373-3394. [Abstract]

Western blot analysis on p-Akt, Akt, p-mTOR and mTOR in control PASMCs and PASMCs treated with PDGF in the absence (vehicle control, Veh) and presence (Halofuginone; HF) of 1 μM halofuginone (for 24 h).
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Tissue Eng Regen Med

Three-Dimensional Modeling of the Structural Microenvironment in Post-Traumatic War Wounds. [Abstract]

2021 Dec;18(6):963-973. PMID: 34363599
ACS Infect Dis

Human Polo-like Kinase Inhibitors as Antiplasmodials. [Abstract]

2023 Apr 14;9(4):1004-1021. PMID: 36919909
iScience

EtcPRS Mut as a molecular marker of halofuginone resistance in Eimeria tenella and Toxoplasma gondii. [Abstract]

2023 Mar 4;26(4):106334. PMID: 36968087
Antiviral Res

Repurposing screen using a robust human rhinovirus infectious clone identifies pyrvinium pamoate with antiviral activity. [Abstract]

2026 Jun:250:106417. PMID: 42025967
RNA

Tuning tRNA synthetase inhibition reveals parabolic induction of stress granules limited in size and RNA content. [Abstract]

2026 Feb 8:rna.080883.125. PMID: 41656003
Fish Shellfish Immunol

Loss of Gcn2 exacerbates gossypol induced oxidative stress, apoptosis and inflammation in zebrafish. [Abstract]

2024 Aug:151:109727. PMID: 38936520
J Virol

Febrifugine dihydrochloride restricts porcine epidemic diarrhea virus replication by modulating the IGF1R-driven PI3K/AKT-apoptosis axis. [Abstract]

2026 May 19;100(5):e0011726. PMID: 41983768
J Funct Foods

2024 Jul.

Halofuginone hydrochloride purchased from MedChemExpress. Usage Cited in: J Funct Foods. 2024 Jul.

Cell viability measured by MTT assay after treatment with 100, 200, 400, 800, and 1000 nM concentrations of Halofuginone (HF) in parental cells MDA-MB-231 and BT-20 for 24 h, as well as resistant cells MDA-MB-231/PR and BT-20/PR.

Halofuginone hydrochloride purchased from MedChemExpress. Usage Cited in: J Funct Foods. 2024 Jul.

Halofuginone (HF; 200 nM; 24 h) treated MDA-MB-231/PR and BT20/PR cells reduced cell invasion capabilities.
Photodiagnosis Photodyn Ther

Halofuginone enhances the anti-tumor effect of ALA-PDT by suppressing NRF2 signaling in cSCC. [Abstract]

2022 Mar:37:102572. PMID: 34628069
Indian J Hematol Blood Transfus

Halofuginone Inhibits Osteoclastogenesis and Enhances Osteoblastogenesis by Regulating Th17/Treg Cell Balance in Multiple Myeloma Mice with Bone Lesions. [Abstract]

2024 Jul;40(3):407-414. PMID: 39011260
bioRxiv

2025 July 11.
Rutgers University

2025.
bioRxiv

2025 April 12.
Friedrich-Alexander University Erlangen-Nuremberg

2023 May 2.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (279 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Tsuchida K, et al. Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Free Radic Biol Med. 2017 Feb;103:236-247. [Content Brief]

[2]. Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7. [Content Brief]

[3]. Cui Z, et al. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone. Ann Rheum Dis. 2016 Sep;75(9):1714-21. [Content Brief]

[4]. Tracy L McGaha, et al. Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts. J Invest Dermatol. 2002 Mar;118(3):461-70. [Content Brief]

[5]. Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Halofuginone hydrochloride

20 Cited Publications

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Halofuginone hydrochloride