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  2. Virus Protease HSV HIV Flavivirus
  3. Theaflavin 3,3'-digallate

Theaflavin 3,3'-digallate  (Synonyms: TF-3; ZP10)

Cat. No.: HY-N1992 Purity: 99.73%
Handling Instructions Technical Support

Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent.

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

CAS No. : 30462-35-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Theaflavin 3,3'-digallate:

Top Publications Citing Use of Products

    Theaflavin 3,3'-digallate purchased from MedChemExpress. Usage Cited in: Autophagy. 2024 Dec;20(12):2769-2784.  [Abstract]

    HeLa cells were transfected with WT NS2B3 or its protease-deficient mutant (S135A) for 24 h. Subsequently, the cells were treated with TF-3 (Theaflavin 3,3'-digallate: 25 μM) or PBS for an additional 24 h. After treatment, cell lysates were analyzed by western blot to detect endogenous SQSTM1 cleavage using anti-SQSTM1 antibodies.

    Theaflavin 3,3'-digallate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Mar 23:12:648969.  [Abstract]

    TFDG (Theaflavin 3,3'-digallate: 1/10 mg/kg) promoted trabecular bone formation in ovariectomized (OVX) mice. H&E staining of bone tissue.

    Theaflavin 3,3'-digallate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Mar 23:12:648969.  [Abstract]

    TFDG (Theaflavin 3,3'-digallate: 1/10 mg/kg) promotes the expression of osteogenic markers in vivo. Representative immunohistochemical staining of OCN and Runx2 in decalcified bone sections.

    Theaflavin 3,3'-digallate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Mar 23:12:648969.  [Abstract]

    CCK8 assay was used to detect the effects of different concentrations of TFDG (Theaflavin 3,3'-digallate) and different intervention times on MC3T3-E1 cells.

    Theaflavin 3,3'-digallate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Mar 23:12:648969.  [Abstract]

    MC3T3-E1 cells were cultured for 7 days in osteogenic media containing or without 10 ng/ml TNF-α and different concentrations of TFDG (Theaflavin 3,3'-digallate: 0.1 μM for low-dose group and 1 μM for high-dose group). Western blot results were obtained.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Theaflavin 3,3'-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC50 of 2.3 μM. Theaflavin 3,3'-digallat directly binds to ZIKVpro (Kd=8.86 μM) and inhibits ZIKV replication. Theaflavin 3,3'-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1[1]. Theaflavin 3,3'-digallate, the typical pigment in black tea, is a potent antitumor agent[2].

    IC50 & Target[1]

    HSV

     

    HIV-1

     

    Cellular Effect
    Cell Line Type Value Description References
    H9 IC50
    48 μg/mL
    Compound: 38
    Inhibition of uninfected H9 lymphocytic cell growth
    Inhibition of uninfected H9 lymphocytic cell growth
    10.1016/0960-894X(96)00095-9
    HCT-116 IC50
    120.5 μM
    Compound: Page no 9, R20C2
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 37776575]
    In Vitro

    Theaflavin 3,3'-digallate (TF-3; 6.25, 12.5, 25 μM; 24 hours) markedly reduces viral RNA copy numbers and NS3, U87 MG protein expression in a dose-dependent manner[1].
    Theaflavin 3,3'-digallate inhibits dose-dependently ZIKV replication in Vero E6 cells (EC50=7.65 μM). Theaflavin 3,3'-digallate has minor cytotoxicity up to 40 μM in Vero E6 cells. Theaflavin 3,3'-digallate can inhibit the post-entry events of the ZIKV replication cycle from gene transcription and translation levels[1].
    Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM[2].

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

    Western Blot Analysis[1]

    Cell Line: Vero E6 cells
    Concentration: 6.25, 12.5, 25 μM
    Incubation Time: 24 hours
    Result: Markedly reduced NS3, U87 MG protein expression in a dose-dependent manner.
    Clinical Trial
    Molecular Weight

    868.70

    Formula

    C43H32O20

    CAS No.
    Appearance

    Solid

    Color

    Brown to red

    SMILES

    O=C(C1=CC(O)=C(C(O)=C1)O)O[C@H]2[C@H](OC3=CC(O)=CC(O)=C3C2)C4=C5C(C(C(O)=CC([C@@H]6[C@@H](CC7=C(O)C=C(O)C=C7O6)OC(C8=CC(O)=C(C(O)=C8)O)=O)=C5)=O)=C(C(O)=C4)O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, sealed storage, away from moisture and light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (115.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 100 mg/mL (115.11 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1511 mL 5.7557 mL 11.5115 mL
    5 mM 0.2302 mL 1.1511 mL 2.3023 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 and light). 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (5.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.73%

    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 and light). 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
    DMSO / H2O 1 mM 1.1511 mL 5.7557 mL 11.5115 mL 28.7786 mL
    5 mM 0.2302 mL 1.1511 mL 2.3023 mL 5.7557 mL
    10 mM 0.1151 mL 0.5756 mL 1.1511 mL 2.8779 mL
    15 mM 0.0767 mL 0.3837 mL 0.7674 mL 1.9186 mL
    20 mM 0.0576 mL 0.2878 mL 0.5756 mL 1.4389 mL
    25 mM 0.0460 mL 0.2302 mL 0.4605 mL 1.1511 mL
    30 mM 0.0384 mL 0.1919 mL 0.3837 mL 0.9593 mL
    40 mM 0.0288 mL 0.1439 mL 0.2878 mL 0.7195 mL
    50 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5756 mL
    60 mM 0.0192 mL 0.0959 mL 0.1919 mL 0.4796 mL
    80 mM 0.0144 mL 0.0719 mL 0.1439 mL 0.3597 mL
    100 mM 0.0115 mL 0.0576 mL 0.1151 mL 0.2878 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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    • 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.

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    Product Name:
    Theaflavin 3,3'-digallate
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