Theaflavin 3,3'-digallate
Based on 9 publication(s) in Google Scholar
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.
- Purity: 99.89%
- CAS No.: 30462-35-2
- Formula: C43H32O20
- Molecular Weight:868.70
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Theaflavin 3,3'-digallate
More- Autophagy. 2024 Dec;20(12):2769-2784. [Abstract]
- Genes Dis. 2026 Mar 12.
- Int J Food Microbiol. 2026 Apr 16:451:111668. [Abstract]
- Food Microbiol. 2026 Jun:136:105016. [Abstract]
- Front Pharmacol. 2021 Mar 23:12:648969. [Abstract]
- Microbiol Spectr. 2023 Sep 21;11(5):e0267123. [Abstract]
- Vet Microbiol. 2026 May:316:110992. [Abstract]
- Exp Ther Med. 2022 Jan;23(1):11. [Abstract]
- bioRxiv. 2023 Jan 31.
Customer Validation & Images
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WB
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Histological Imaging/Staining
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IHC
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Cell Proliferation/Viability Assay
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WB
Biological Activity
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HSV |
HIV-1 |
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Cell Line
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Type | Value | Description | References |
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| H9 | IC50 |
48 μg/mL
Compound: 38
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Inhibition of uninfected H9 lymphocytic cell growth
Inhibition of uninfected H9 lymphocytic cell growth
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10.1016/0960-894X(96)00095-9 |
| HCT-116 | IC50 |
120.5 μM
Compound: Page no 9, R20C2
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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
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[PMID: 37776575] |
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.
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Cell Line:Vero E6 cells
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Concentration:6.25, 12.5, 25 μM
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Incubation Time:24 hours
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Result:Markedly reduced NS3, U87 MG protein expression in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 30462-35-2
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Appearance Solid
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Molecular Weight 868.70
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Formula C43H32O20
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Color Brown to red
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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
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Synonyms
TF-3; ZP10
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (9)
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Journal Impact Factor
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Most Recent
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Autophagy
Cleavage of SQSTM1/p62 by the Zika virus protease NS2B3 prevents autophagic degradation of viral NS3 and NS5 proteins. [Abstract]2024 Dec;20(12):2769-2784. PMID: 39128850
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.
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Int J Food Microbiol
Synergistic action of ε-polylysine and theaflavin-3,3'-digallate against Hafnia alvei in turbot preservation: Quorum sensing disruption and bacterial sensitization. [Abstract]2026 Apr 16:451:111668. PMID: 41687313 -
Food Microbiol
Shelf-life extension of turbot using theaflavin-3,3'-digallate: A growth-neutral quorum sensing inhibitor targeting Hafnia alvei. [Abstract]2026 Jun:136:105016. PMID: 41478691 -
Front Pharmacol
Theaflavin-3,3'-Digallate Promotes the Formation of Osteoblasts Under Inflammatory Environment and Increases the Bone Mass of Ovariectomized Mice. [Abstract]2021 Mar 23:12:648969. PMID: 33833684
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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Microbiol Spectr
Potential quorum-sensing inhibitor of Hafnia alvei H4-theaflavin-3,3´-digallate analyzed by virtual screening and molecular simulation. [Abstract]2023 Sep 21;11(5):e0267123. PMID: 37732782 -
Vet Microbiol
The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]2026 May:316:110992. PMID: 41865607 -
Exp Ther Med
Theaflavin-3,3'-digallate attenuates cigarette smoke extract-induced pulmonary emphysema in mice by suppressing necroptosis. [Abstract]2022 Jan;23(1):11. PMID: 34815763 -
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Xiangling Cui, et al. Identification of Theaflavin-3,3'-Digallate as a Novel Zika Virus Protease Inhibitor. Front Pharmacol. 2020 Oct 21;11:514313. [Content Brief]
[2]. Ding Y, et al. Pre-treated theaflavin-3,3'-digallate has a higher inhibitory effect on the HCT116 cell line. Food Nutr Res. 2017 Nov 15;61(1):1400340. [Content Brief]
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 |
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| 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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