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  3. Homoharringtonine

Homoharringtonine  (Synonyms: HHT; Omacetaxine mepesuccinate; ホモハリントニン)

製品番号: HY-14944 純度: 99.75%
COA 取扱説明書 Technical Support

Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

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Homoharringtonine 構造式

Homoharringtonine 構造式

CAS 番号 : 26833-87-4

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無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
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10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 84 在庫あり
Solid
5 mg USD 70 在庫あり
10 mg USD 138 在庫あり
25 mg USD 276 在庫あり
50 mg USD 390 在庫あり
100 mg USD 550 在庫あり
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カスタマーレビュー

Based on 29 publication(s) in Google Scholar

Other Forms of Homoharringtonine:

Top Publications Citing Use of Products

    Homoharringtonine purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 6;8(23):37594-37604.  [Abstract]

    The expression of apoptosis proteins. K562/G01 cells treated with HHT 0, 50nM, 100 nM, 200nM for 24h. Bcl-2, caspase9, caspase3 express.

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    製品説明

    Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

    IC50 & Target[1]

    STAT3

     

    Cellular Effect
    Cell Line Type Value Description References
    4T1 IC50
    0.06 μM
    Compound: 1; HHT
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    A204 IC50
    0.004 μM
    Compound: 1; HHT
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human A204 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    A549 IC50
    0.03 μM
    Compound: Homoharringtonine
    Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method
    Cytotoxicity against human A549 cells assessed as reduction of cell growth by SRB method
    [PMID: 18782668]
    A549 IC50
    18.28 nM
    Compound: HHT
    Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay
    Inhibition of Nuclear factor erythroid 2-related factor 2 5'-untranslated region guanine-rich DNA sequence in human A549 cells harboring ARE-GFP-Luc assessed as reduction in ARE-luciferase activity after 24 hrs by firefly luciferase reporter gene assay
    [PMID: 31270017]
    A549 IC50
    31.6 nM
    Compound: homoharringtonine
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 31916761]
    BaF3 IC50
    0.081 μM
    Compound: 1; HHT
    Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing Bcr/Abl-T315I mutant assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    Caco-2 CC50
    1.72 μM
    Compound: HOMOHARRINGTONINE
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
    10.21203/rs.3.rs-23951/v1
    Caco-2 IC50
    4.71 μM
    Compound: HOMOHARRINGTONINE
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
    10.21203/rs.3.rs-23951/v1
    HCT-116 IC50
    0.013 μM
    Compound: 1; HHT
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    HeLa IC50
    0.4 μM
    Compound: Homoharringtonine
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    [PMID: 33905250]
    HeLa IC50
    1.7 μM
    Compound: HHT
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    [PMID: 35148094]
    HepG2 IC50
    34.5 nM
    Compound: homoharringtonine
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 31916761]
    HL-60 IC50
    0.013 μM
    Compound: 1; HHT
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    HL-60 IC50
    0.02 μM
    Compound: homoharringtonine
    Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
    Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
    10.1039/C0MD00241K
    HL-60 IC50
    0.022 μM
    Compound: HHT
    Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay
    Antiproliferative activity against human HL60 cells after 62 hrs by MTS assay
    [PMID: 29286665]
    HL-60 IC50
    21.8 nM
    Compound: HHT
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth measured after 68 hrs by MTS assay
    [PMID: 35148094]
    Huh-7 IC50
    0.04 μM
    Compound: 1; HHT
    Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    K562 IC50
    0.014 μM
    Compound: 1; HHT
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    KB IC50
    0.004 μM
    Compound: Homoharringtonine
    Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method
    Cytotoxicity against human KB cells assessed as reduction of cell growth by SRB method
    [PMID: 18782668]
    L02 IC50
    0.064 μM
    Compound: 1; HHT
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MDA-MB-453 IC50
    0.021 μM
    Compound: 1; HHT
    Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MOLT-4 IC50
    0.007 μM
    Compound: 1; HHT
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    MV4-11 IC50
    0.005 μM
    Compound: 1; HHT
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H1299 IC50
    0.022 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H1975 IC50
    0.022 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    NCI-H716 IC50
    0.065 μM
    Compound: 1; HHT
    Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H716 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    OCI-Ly3 IC50
    0.005 μM
    Compound: 1; HHT
    Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human OCILY3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    U-937 IC50
    0.012 μM
    Compound: 1; HHT
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay
    [PMID: 36242991]
    体外実験

    Homoharringtonine inhibits IL-6-induced STAT3 phosphorylation in a dose- and time-dependent manner. Homoharringtonine (HHT) inhibits cells growth, cell viability and colony formation, as well as induced cell apoptosis through mitochondria pathway. The cytotoxicity of Homoharringtonine on human NSCLC cell lines is investigated, A549 (wild type EGFR) and NCI-H1975 (H1975, mutant EGFR with L858R and T790M), Gefitinib is used as a control. By MTT assay, Homoharringtonine has moderate cytotoxicity to A549 with an IC50 of 3.7 μM and H1975 cells are more sensitive to Homoharringtonine with an IC50 of 0.7 μM. Homoharringtonine inhibits the cell proliferation and growth of A549 cells and H1975 cells in a time- and dose-dependent manner through MTT assay. By trypan blue exclusion assay, Homoharringtonine rapidly reduces viable A549 and H1975 cells in a dose- and time-dependent manner. Homoharringtonine significantly inhibits the clonogenic ability of A549 and H1975 cells[1].

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

    体内実験

    Homoharringtonine (10 mg/kg; 5 times weekly; 3 weeks) exhibits antitumor activity in H1975 xenograft nude mouse models[1].
    Homoharringtonine (1 mg/kg; subcutaneous injection; twice daily; 7 days) shows antitumor activity in MDA-MB-231 xenograft nude mouse models[2].

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

    Animal Model: Nude immunodeficient mice aged 6-8 weeks old treated H1975 cells[1]
    Dosage: 10 mg/kg
    Administration: 5 times per week; 3 weeks
    Result: Significantly repressed tumor growth, and there was no apparent side effect as indicated by no reduction in mice body weight.
    Downregulated the phosphorylation of STAT3 and the expression of MCL1 in tumor tissues.
    Animal Model: Swiss nu/nu female mice aged 6 weeks old treate MDA-MB-231 cells[1]
    Dosage: 1 mg/kg
    Administration: Subcutaneous injection (s.c.); bi-daily; 7 days.
    Result: Reduced the mean tumor volume by 36.5% in the treated group compared to the control group at day 10, with minimal change in animal weight, indicating significant tumor growth inhibition without general toxicity.
    臨床実験
    分子量

    545.62

    Synonyms

    HHT; Omacetaxine mepesuccinate; ホモハリントニン

    分子式

    C29H39NO9

    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    [H][C@@]12[C@](CCC3)(C=C(OC)[C@]2(OC([C@](CCCC(O)(C)C)(O)CC(OC)=O)=O)[H])N3CCC4=CC5=C(OCO5)C=C14

    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 50 mg/mL (91.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1.4 mg/mL (2.57 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8328 mL 9.1639 mL 18.3278 mL
    5 mM 0.3666 mL 1.8328 mL 3.6656 mL
    10 mM 0.1833 mL 0.9164 mL 1.8328 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * 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

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    一般には略語で表示されます:C1V1 = C2V2

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    体内:

    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 (4.58 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 (4.58 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 1.67 mg/mL (3.06 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Please enter your animal formula composition:
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    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, 1 year; -20°C, 6 months (protect from light)

    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.
    純度とドキュメンテーション

    純度: 99.96%

    参考文献

    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.8328 mL 9.1639 mL 18.3278 mL 45.8194 mL
    DMSO 5 mM 0.3666 mL 1.8328 mL 3.6656 mL 9.1639 mL
    10 mM 0.1833 mL 0.9164 mL 1.8328 mL 4.5819 mL
    15 mM 0.1222 mL 0.6109 mL 1.2219 mL 3.0546 mL
    20 mM 0.0916 mL 0.4582 mL 0.9164 mL 2.2910 mL
    25 mM 0.0733 mL 0.3666 mL 0.7331 mL 1.8328 mL
    30 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
    40 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1455 mL
    50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9164 mL
    60 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
    80 mM 0.0229 mL 0.1145 mL 0.2291 mL 0.5727 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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      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.

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    製品名:
    Homoharringtonine
    製品番号:
    HY-14944
    数量:
    MCE 日本正規代理店: