2. Metabolic Enzyme/Protease NF-κB Apoptosis
  3. MMP NF-κB Apoptosis TNF Receptor
  4. TAPI-1

TAPI-1 is a broad-spectrum MMP inhibitor and NF-κB p65 inhibitor that targets ADAM17/TACE, ADAM10 and other proteins. TAPI-1 reduces the proteolytic cleavage of membrane-bound TNF-α, decreases TNF-α levels, inhibits NF-κB pathway activation, and downregulates profibrotic markers. TAPI-1 reduces the proportion of proinflammatory immune cells, alleviates cardiac and airway fibrosis, and improves cardiac function after myocardial infarction. Meanwhile, TAPI-1 inhibits the viability, migration and invasion of esophageal squamous cell carcinoma cells, enhances the chemosensitivity of Cisplatin (HY-17394), induces apoptosis, and shows low toxicity to normal esophageal epithelial cells. TAPI-1 can be widely used in studies related to myocardial infarction-induced heart failure, severe traumatic tracheal stenosis, esophageal squamous cell carcinoma and other conditions.

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

CAS No. : 163847-77-6

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Based on 15 publication(s) in Google Scholar

Other Forms of TAPI-1:

TAPI-1 Related Antibodies

Top Publications Citing Use of Products

    TAPI-1 purchased from MedChemExpress. Usage Cited in: Cell Syst. 2025 Mar 19;16(3):101203.  [Abstract]

    Quantification of peak radial velocity (left) and migration zone width (right) at 4 h post illumination for illuminated tissues treated with each compound. N=6,5,6 tissues for control, TAPI-1 (10 μM), and N-blebbistatin, respectively.

    TAPI-1 purchased from MedChemExpress. Usage Cited in: MedComm. 2023 Jul 8;4(4):e320.  [Abstract]

    With TAPI-1 (1 μM) treatment, mTIMD4 protein expression increased whiles sTIMD4 level decreased noticeably.

    TAPI-1 purchased from MedChemExpress. Usage Cited in: MedComm. 2023 Jul 8;4(4):e320.  [Abstract]

    With TAPI-1 (1 μM) treatment, mTIMD4 protein expression increased whiles sTIMD4 level decreased noticeably.

    TAPI-1 purchased from MedChemExpress. Usage Cited in: MedComm. 2023 Jul 8;4(4):e320.  [Abstract]

    TAPI-1 (1 μM) abolished the protein expression of phosphorylated nuclear factor kappa B (p-NF-κB), anti-Toll-like receptor 4 (TLR-4) and IL‐6 that were upregulated by ox-LDL.

    TAPI-1 purchased from MedChemExpress. Usage Cited in: MedComm. 2023 Jul 8;4(4):e320.  [Abstract]

    RAW264.7 cells were treated with LPS (1 μg/mL) and TAPI-1 (1 μM) for 24 h, and the protein expression of mTIMD4, sTIMD4 by Western blotting.

    View All MMP Isoform Specific Products:

    View All Isoforms
    MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

    View All NF-κB Isoform Specific Products:

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    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

    View All TNF Receptor Isoform Specific Products:

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    TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TAPI-1 is a broad-spectrum MMP inhibitor and NF-κB p65 inhibitor that targets ADAM17/TACE, ADAM10 and other proteins. TAPI-1 reduces the proteolytic cleavage of membrane-bound TNF-α, decreases TNF-α levels, inhibits NF-κB pathway activation, and downregulates profibrotic markers. TAPI-1 reduces the proportion of proinflammatory immune cells, alleviates cardiac and airway fibrosis, and improves cardiac function after myocardial infarction. Meanwhile, TAPI-1 inhibits the viability, migration and invasion of esophageal squamous cell carcinoma cells, enhances the chemosensitivity of Cisplatin (HY-17394), induces apoptosis, and shows low toxicity to normal esophageal epithelial cells. TAPI-1 can be widely used in studies related to myocardial infarction-induced heart failure, severe traumatic tracheal stenosis, esophageal squamous cell carcinoma and other conditions[1][2][3].

    IC50 & Target

    ADAM17

     

    ADAM10

     

    In Vitro

    TAPI-1 (1.25-20 μM; 24-72 h) inhibits viability of TE-1 and Eca109 ESCC cells in a dose- and time-dependent manner without affecting viability of normal Het-1A esophageal epithelial cells[3].
    TAPI-1 (10 μM; 24 h) upregulates TRAIL mRNA in TE-1 ESCC cells but does not alter apoptosis-related gene expression in Eca109 ESCC cells; TAPI-1 (5 μM; 12 h) downregulates multiple Cisplatin (HY-17394) resistance-related genes in both TE-1 and Eca109 ESCC cells[3].
    TAPI-1 (10 μM; 72 h) does not induce apoptosis in TE-1 or Eca109 ESCC cells, but TAPI-1 (5 μM; 48 h) enhances cisplatin-induced apoptosis in both TE-1 and Eca109 ESCC cells[3].
    TAPI-1 (5 μM; 48 h) enhances the sensitivity of TE-1 and Eca109 ESCC cells to cisplatin, as shown by significantly reduced cisplatin IC50 values[3].
    TAPI-1 (10 μM; 12 h) suppresses NF-κB signaling in TE-1 and Eca109 ESCC cells by reducing NF-κB p65 phosphorylation and nuclear translocation[3].

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

    TAPI-1 Related Antibodies

    Cell Viability Assay[3]

    Cell Line: human esophageal squamous cell carcinoma (ESCC) TE-1, Eca109 cells; human normal esophageal epithelial Het-1A cells
    Concentration: 1.25-20 μM (24 h viability assay); 10 μM (time-course viability assay)
    Incubation Time: 24 h (dose-response); 24, 48, 72 h (10 μM time-course)
    Result: Inhibited viability of TE-1 and Eca109 cells in a dose-dependent manner, with significant decreases observed at 10 and 20 μM after 24 h.
    Reduced viability of TE-1 and Eca109 cells significantly at 24 and 48 h at 10 μM, with no further change at 72 h.
    Caused no significant viability changes in Het-1A cells across any tested concentration or time point.

    Real Time qPCR[3]

    Cell Line: ESCC TE-1, Eca109 cells
    Concentration: 10 μM (apoptosis-related gene assay); 5 μM (cisplatin resistance-related gene assay)
    Incubation Time: 24 h (apoptosis-related gene assay); 12 h (cisplatin resistance-related gene assay)
    Result: Upregulated pro-apoptosis TRAIL mRNA significantly in TE-1 cells at 10 μM for 24 h, with no changes in BIM or BCL2 mRNA levels.
    Caused no significant changes in BIM, TRAIL, or BCL2 mRNA levels in Eca109 cells at 10 μM for 24 h.
    Downregulated 29 cisplatin resistance-related genes in TE-1 cells at 5 μM for 12 h.
    Downregulated 21 cisplatin resistance-related genes in Eca109 cells at 5 μM for 12 h, with 20 genes downregulated in both cell lines.
    In Vivo

    TAPI-1 delivered via neutrophil-mimic liposomal nanoparticles (TAPI-1-Neu-LNPs) (50 µg; i.v. via tail vein; every other day; 4 weeks) significantly improves left ventricular function, mitigates cardiac remodelling, reduces cardiac fibrosis, and attenuates inflammatory immune cell infiltration in rats with myocardial infarction, with superior efficacy compared to untargeted TAPI-1 (50 µg; i.v. via tail vein; every other day; 4 weeks)[1].
    TAPI-1 (0.8 mg/mL; local tracheal spray; once weekly; 3 weeks), either alone or combined with a silicone stent, significantly alleviates severe traumatic tracheal stenosis in Beagle dogs by inhibiting the ADAM17/TGF-β1 pathway, with TAPI-1 alone achieving the lowest degree of tracheal stenosis[2].

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

    Animal Model: Beagle (male, 12 months old, 10-12 kg, traumatic tracheal stenosis model established via rigid bronchoscope-guided argon plasma coagulation + balloon compression)[2]
    Dosage: 0.8 mg/mL (1 mL volume)
    Administration: local tracheal spray; once weekly; 3 weeks (initiated first week post-modeling); silicone stent implantation (third week post-modeling, for combined group)
    Result: Significantly reduced tracheal stenosis degree.
    Significantly downregulated tracheal mRNA and protein levels of ADAM17, TGF-β1, and fibronectin 1, with levels lower than those in the mitomycin treatment group.
    Alleviated pathological tracheal changes including reduced airway epithelial hyperplasia, submucosal thickening, fibrous tissue proliferation, and lymphocytic infiltration.
    When combined with silicone stent, significantly reduced tracheal stenosis degree, with no significant difference compared to TAPI-1 alone group.
    When combined with silicone stent, significantly downregulated tracheal mRNA and protein levels of ADAM17, TGF-β1, and fibronectin 1, but levels were significantly higher than those in the TAPI-1 alone group.
    When combined with silicone stent, alleviated pathological tracheal changes including reduced airway epithelial hyperplasia, submucosal thickening, fibrous tissue proliferation, and lymphocytic infiltration.
    Molecular Weight

    499.60

    Formula

    C26H37N5O5
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N[C@@H](CC1=CC=C2C=CC=CC2=C1)C(N[C@@H](C)C(NCCN)=O)=O)[C@H](CC(C)C)CC(NO)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (200.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0016 mL 10.0080 mL 20.0160 mL
    5 mM 0.4003 mL 2.0016 mL 4.0032 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    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).
    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: 99.36%

    SDS (479 KB)

    COA (247 KB) HNMR (311 KB) RP-HPLC (240 KB) LCMS (84 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0016 mL 10.0080 mL 20.0160 mL 50.0400 mL
    5 mM 0.4003 mL 2.0016 mL 4.0032 mL 10.0080 mL
    10 mM 0.2002 mL 1.0008 mL 2.0016 mL 5.0040 mL
    15 mM 0.1334 mL 0.6672 mL 1.3344 mL 3.3360 mL
    20 mM 0.1001 mL 0.5004 mL 1.0008 mL 2.5020 mL
    25 mM 0.0801 mL 0.4003 mL 0.8006 mL 2.0016 mL
    30 mM 0.0667 mL 0.3336 mL 0.6672 mL 1.6680 mL
    40 mM 0.0500 mL 0.2502 mL 0.5004 mL 1.2510 mL
    50 mM 0.0400 mL 0.2002 mL 0.4003 mL 1.0008 mL
    60 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8340 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6255 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5004 mL
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    TAPI-1 Related Classifications

    Help & FAQs
    • 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:

    TAPI-1163847-77-6TAPI1TAPI 1MMPNF-κBApoptosisTNF ReceptorMatrix metalloproteinasesNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFResophageal squamous cell carcinoma cellsNF-κB p65ADAM10TNF-αTE-1Het-1AMMPsmyocardial infarction modelsADAM17/TACEEca109Inhibitorinhibitorinhibit

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