1. NF-κB
    Autophagy
  2. NF-κB
    Autophagy

Dihydroartemisinin (Synonyms: β-Dihydroartemisinin; DHA; Dihydroqinghaosu)

Cat. No.: HY-N0176 Purity: >99.0%
Handling Instructions

Dihydroartemisinin inhibits NF-κB activity by blocking RelA/p65 translocation to the nucleus. Dihydroartemisinin activates autophagy induction in tumor cells.

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

Dihydroartemisinin Chemical Structure

Dihydroartemisinin Chemical Structure

CAS No. : 71939-50-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 60 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 84 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg USD 108 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
500 mg USD 156 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
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Customer Review

    Dihydroartemisinin purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jun 27;501(3):636-642.

    Immunoblot analysis of the expression levels of BCL-2 and BAX after treatment of HCT116 TP53-/- cells with 20 μM 5-FU and 1.25 μM DHA alone or in combination for 48 h. Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) served as a loading control.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dihydroartemisinin inhibits NF-κB activity by blocking RelA/p65 translocation to the nucleus. Dihydroartemisinin activates autophagy induction in tumor cells.

    IC50 & Target[1]

    RelA

     

    Autophagy

     

    In Vitro

    Dihydroartemisinin (DHA) is an antimalarial agent. Dihydroartemisinin treatment effectively up-regulates the cytosolic RelA/p65 protein level and down-regulates the nuclear RelA/p65 protein level. Dihydroartemisinin blocks the nuclear translocation of RelA/p65 from the cytosol rather than suppressing RelA/p65 protein synthesis. Dihydroartemisinin induces autophagy in RPMI 8226 cells. Dihydroartemisinin suppresses NF-κB activation in RPMI 8226 cells. The NF-κB Dihydroartemisinin -binding activity is examined by EMSA assay. RPMI 8226 cells are exposed to various concentrations of Dihydroartemisinin (10, 20 and 40 μM) for 12 h, and TNF-α is introduced as a positive control for NF-κB activation. Dihydroartemisinin suppresses NF-κB activation in a dose-dependent manner in contrast with TNF-α[1]. Dihydroartemisinin (DHA) can enhance the anti-tumor effect of photodynamic therapy (PDT) on esophageal cancer cells, and cell viability is investigated using the MTT assay. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80 μM), PDT (25 and 20 J/cm2, respectively) or their combination. Single treatment with Dihydroartemisinin or PDT causes a 37±5% or 34±6% reduction in viability in Eca109 cells and a 33±7% or 34±6% reduction in Ec9706 cells, respectively. However, when PDT is combined with Dihydroartemisinin, the cell viability is reduced 59±6% or 61±7% in the cell lines, respectively[2].

    In Vivo

    Single oral doses of Dihydroartemisinin (at 200, 300, 400 or 600 mg/kg), given once on each of day 6-8 post-infection, reduce total-worm burdens by 69.2%-90.6% and female-worm burdens by 62.2%-92.2%, depending on dosage in the first experiment. Similar treatments given on day 34-36 post-infection reduce total-worm burdens by 73.9%-85.5% and female-worm burdens by 83.8%-95.3%[3].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 3.5168 mL 17.5840 mL 35.1679 mL
    5 mM 0.7034 mL 3.5168 mL 7.0336 mL
    10 mM 0.3517 mL 1.7584 mL 3.5168 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    To determine NF-κB Dihydroartemisinin-binding activity, an electrophoretic mobility shift assay (EMSA) is performed. Nuclear extracts are prepared and incubated with 32P-end-labeled 45-mer double-stranded oligonucleotide (15 μg protein with 16 fmol DNA) from the HIV long terminal repeat, 5′-TTGTTACAAGGGACTTTCCGCTG GGGACTTTCCAGGGAGGCGTGG-3′ (boldface indicates NF-κB binding sites), for 30 min at 37 °C. The Dihydroartemisinin-protein complex formed is separated from free oligonucleotide on 6.6% native polyacrylamide gels. A double-stranded mutated oligonucleotide, 5′-TTGTTACAA CTCACTTTCCGCTGCTCACTTTCCAGGGAGGCGTGG-3′, is used to examine binding specificity of NF-κB to the DNA. The binding specificity is also examined by competition with the unlabeled oligonucleotide. Preimmune serum (PIS) is included as a negative control. The dried gels are visualized with a Storm 820, and radioactive bands are quantified using Imagequant software[1].
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    Eca109 (4×103 cells/well) and Ec9706 (5×103 cells/well) cells are grown in 96-well plates and cultured overnight to allow for cell attachment. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80 μM), PDT (25 and 20 J/cm2, respectively) or their combination. After incubation for 24h, MTT (20 μL) is added to each well and incubated for 4 h at 37°C. Formazan crystals are dissolved in 150 μL of DMSO for 10 min with shaking. The absorbance is measured at 490 nm on a plate reader, and the experiment is repeated three times[2].
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Dihydroartemisinin is prepared in DMSO, Tween-80 and distilled water to give aqueous solutions[3].

    Mice[3]
    Mice of the Kunming strain, each weighing 20-24 g, are used. In the first experiment, design to investigate the effect of multiple doses of Dihydroartemisinin on the schistosomula and adult worms of S. japonicum, mice are given three daily doses, of 200, 300, 400 or 600 mg Dihydroartemisinin/kg (in dose volumes of 25 mL/kg), on days 6-8 or 34-36 post-infection, respectively. An additional group of mice, infected but not given the drug, serve as a control.
    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    284.35

    Formula

    C₁₅H₂₄O₅

    CAS No.

    71939-50-9

    SMILES

    O[[email protected]@H]1[[email protected]](C)[[email protected]]2([H])CC[[email protected]@H](C)[[email protected]]3([H])CC[[email protected]@](O4)(C)OO[[email protected]]32[[email protected]]4([H])O1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 18.67 mg/mL (Need ultrasonic and warming)

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: >99.0%

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    Product Name:
    Dihydroartemisinin
    Cat. No.:
    HY-N0176
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