2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Anti-infection Membrane Transporter/Ion Channel Neuronal Signaling
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  4. Halofuginone hydrobromide

Halofuginone hydrobromide  (Synonyms: RU-19110 hydrobromide)

Cat. No.: HY-N1584A Purity: 99.85%
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Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki 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.

For research use only. We do not sell to patients.

CAS No. : 64924-67-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 20 publication(s) in Google Scholar

Other Forms of Halofuginone hydrobromide:

Halofuginone hydrobromide Related Antibodies

Top Publications Citing Use of Products

    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.

    Halofuginone hydrobromide purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Jul 25:143:156788.

    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.

    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.

    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).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki 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

     

    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.

    Halofuginone hydrobromide Related Antibodies

    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.
    Molecular Weight

    495.59

    Formula

    C16H18Br2ClN3O3
    CAS No.
    Appearance

    Solid

    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
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0178 mL 10.0890 mL 20.1780 mL
    5 mM 0.4036 mL 2.0178 mL 4.0356 mL
    View the Complete Stock Solution Preparation Table

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    V2

    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.85%

    SDS (623 KB)

    COA (249 KB) HNMR (291 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * 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.

    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
    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.

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    Halofuginone hydrobromide Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Halofuginone64924-67-0RU-19110RU19110RU 19110DNA/RNA SynthesisTGF-beta/SmadParasiteSodium ChannelCalcium ChannelTransforming growth factor betaNa channelsNa+ channelsCa2+ channelsCa channelstype-Icollagencollagen-1prolyl-tRNAosteoarthritisTGF-βInhibitorinhibitorinhibit

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