Referencia número: HY-N1584A

Halofuginone hydrobromide

(Synonyms: RU-19110 hydrobromide)

22 Cited Publications

Revisión del cliente

Based on 22 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.

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Pureza: 99.85%
No. CAS: 64924-67-0
Fòrmula: C₁₆H₁₈Br₂ClN₃O₃
Peso molecular:495.59

Almacenamiento:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Halofuginone hydrobromide Chemical Structure

No. CAS: 64924-67-0

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM^[1]^[2]. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity^[3]^[4]. 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^[5].

IC₅₀ & Target

Plasmodium

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

Ver todos los productos específicos de isoformas TGF-beta/Smad :

Smad1
Smad3

Ver todos los productos específicos de isoformas Parasite :

Ver todos los productos específicos de isoformas Sodium Channel :

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In Vitro

Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase^[1].
The IC₅₀s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC₅₀s of Halofuginone (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 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) 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.

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 hours
Result:

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

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 nM
Incubation Time:

24 hours
Result:

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

In Vivo

Halofuginone (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 (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 (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 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.

Chemical Information

No. CAS 64924-67-0
Appearance Solid
Peso molecular 495.59
Fòrmula C₁₆H₁₈Br₂ClN₃O₃
Color White to off-white
SMILES

O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3.Br
Synonyms

RU-19110 hydrobromide
Structure Classification
- Alkaloids
- Piperidine Alkaloids
Initial Source
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (22)

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 hydrobromide 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 hydrobromide 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 hydrobromide 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
Hum Gene Ther

Antifibrotic Therapy Augments the Antitumor Effects of Vesicular Stomatitis Virus Via Reprogramming Tumor Microenvironment. [Abstract]

2022 Mar;33(5-6):237-249. PMID: 34405694
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 hydrobromide 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 hydrobromide 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

2026 Jan 15.
bioRxiv

2025 July 11.
Rutgers University

2025.
bioRxiv

2025 April 12.
Friedrich-Alexander University Erlangen-Nuremberg

2023 May 2.

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (100.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.6 mg/mL (5.25 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0178 mL

10.0890 mL

20.1780 mL

5 mM

0.4036 mL

2.0178 mL

4.0356 mL

10 mM

0.2018 mL

1.0089 mL

2.0178 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (281 KB)
SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Instrucciones de manejo (2659 KB)

Referencias

[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]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.0178 mL	10.0890 mL	20.1780 mL	50.4449 mL
H₂O / DMSO	5 mM	0.4036 mL	2.0178 mL	4.0356 mL	10.0890 mL
DMSO	10 mM	0.2018 mL	1.0089 mL	2.0178 mL	5.0445 mL
	15 mM	0.1345 mL	0.6726 mL	1.3452 mL	3.3630 mL
	20 mM	0.1009 mL	0.5044 mL	1.0089 mL	2.5222 mL
	25 mM	0.0807 mL	0.4036 mL	0.8071 mL	2.0178 mL
	30 mM	0.0673 mL	0.3363 mL	0.6726 mL	1.6815 mL
	40 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2611 mL
	50 mM	0.0404 mL	0.2018 mL	0.4036 mL	1.0089 mL
	60 mM	0.0336 mL	0.1681 mL	0.3363 mL	0.8407 mL
	80 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6306 mL
	100 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5044 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Halofuginone hydrobromide

22 Cited Publications

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Halofuginone hydrobromide

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Publications Citing Use of MedChemExpress (MCE) Halofuginone hydrobromide

Ver todos los productos específicos de isoformas DNA/RNA Synthesis

Ver todos los productos específicos de isoformas TGF-beta/Smad

Ver todos los productos específicos de isoformas Parasite

Ver todos los productos específicos de isoformas Sodium Channel

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Actividad biológica

Chemical Information

Publications (22)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Halofuginone hydrobromide Related Classifications

HY-N1584A Related Classifications