TAPI-1
Catalog No.: GC12344Purity:>98%Synonyms: TAPI
TAPI-1 is a TACE (tumor necrosis factor-α converting enzyme) inhibitor that blocks the shedding of the extracellular domain of cell membrane proteins (amphiregulin (AREG)) mediated by TACE by inhibiting its proteolytic activity. TAPI-1 is also a metalloproteinase (MMP) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 163847-77-6
10mM (in 1mL DMSO)In Stock
$653.00
1
1mgIn Stock
$163.00
1
5mgIn Stock
$594.00
1
10mgIn Stock
$1,062.00
1
10mgIn Stock
$1,094.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $653.00 | In Stock | 1 | |
| 1mg | $163.00 | In Stock | 1 | |
| 5mg | $594.00 | In Stock | 1 | |
| 10mg | $1,062.00 | In Stock | 1 | |
| 10mg | $1,094.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
TAPI-1 is a TACE (tumor necrosis factor-α converting enzyme) inhibitor that blocks the shedding of the extracellular domain of cell membrane proteins (amphiregulin (AREG)) mediated by TACE by inhibiting its proteolytic activity[1, 2]. TAPI-1 is also a metalloproteinase (MMP) inhibitor[3]. TAPI-1 can reduce cellular oxidative stress and the production of inflammatory factors[4].
In vitro, TAPI-1 (0-20µM) treatment of TE-1 and Eca109 cells for 24h inhibited cell viability, migration, and invasion in a dose-dependent manner, and promoted cisplatin-induced apoptosis[5]. TAPI-1 (20µM) treatment of A549 cells for 24h reduced cell proliferation and inhibited EGFR and Notch1 mRNA expression[6]. TAPI-1 (5, 10µM) treatment of NCI-H292 cells for 6 and 24h blocked the shedding of amphiregulin (AREG) from the cell membrane stimulated by diacetyl[7].
In vivo, TAPI-1 (10mg/kg) administered by intraperitoneal injection to mice with Staphylococcus aureus-induced arthritis significantly reduced paw swelling and decreased the concentrations of superoxide, nitric oxide, and hydrogen peroxide in joint tissues[8].
References:
[1] Slack B E, Ma L K, Seah C C. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme[J]. Biochemical Journal, 2001, 357(3): 787-794.
[2] Liu C, Xu P, Lamouille S, et al. TACE-mediated ectodomain shedding of the type I TGF-β receptor downregulates TGF-β signaling[J]. Molecular cell, 2009, 35(1): 26-36.
[3] Koon H W, Zhao D, Na X, et al. Metalloproteinases and transforming growth factor-α mediate substance P-induced mitogen-activated protein kinase activation and proliferation in human colonocytes[J]. Journal of Biological Chemistry, 2004, 279(44): 45519-45527.
[4] Bae E H, Kim I J, Choi H S, et al. Tumor necrosis factor α-converting enzyme inhibitor attenuates lipopolysaccharide-induced reactive oxygen species and mitogen-activated protein kinase expression in human renal proximal tubule epithelial cells[J]. The Korean Journal of Physiology & Pharmacology, 2018, 22(2): 135-143.
[5] Gao L, Li L, Zhang D, et al. TAPI-1 exhibits Anti-tumor efficacy in human esophageal squamous cell carcinoma cells via suppression of NF-κB signaling pathway[J]. Digestive Diseases and Sciences, 2024, 69(1): 81-94.
[6] Pancewicz J, Golec P. The effect of TAPI-1 treatment in non-small cell lung cancer cells[J].
[7] Kelly F L, Sun J, Fischer B M, et al. Diacetyl induces amphiregulin shedding in pulmonary epithelial cells and in experimental bronchiolitis obliterans[J]. American journal of respiratory cell and molecular biology, 2014, 51(4): 568-574.
[8] Sultana S, Bishayi B. Potential anti-arthritic and anti-inflammatory effects of TNF-α processing inhibitor-1 (TAPI-1): A new approach to the treatment of S. aureus arthritis[J]. Immunobiology, 2020, 225(2): 151887.
Protocol
| Cell experiment [1]: | |
Cell lines | TE-1、Eca109 cells |
Preparation Method | TE-1 and Eca109 cells were exposed tovarying doses of TAPI-1 (0, 1.25, 2.5, 5, 10, and 20μM) for 24h, following which, cell viability was determined using CCK-8 assay. |
Reaction Conditions | 0, 1.25, 2.5, 5, 10, 20μM; 24h |
Applications | Following exposure of TAPI-1, TE-1, and Eca109 cell viability was inhibited in a dose dependent manner. |
| Animal experiment [2]: | |
Animal models | Adult Swiss albino male mice |
Preparation Method | TAPI-1 was diluted in 5% DMSO in sterile saline solution. The final concentration used was 10mg/kg of body weight. The first dose of TAPI-1 was administered intraperitoneally into each mouse 24h after S.aureus infection and repeated at day 4, day 7, day 10 and day 13 post infection. Control mice received a single dose of TAPI-1 two days prior to sacrifice. |
Dosage form | 10mg/kg; i.p. |
Applications | TAPI-1 administration significantly reduced paw swelling in mice with Staphylococcus aureus-induced arthritis. Following TAPI-1 treatment, the concentrations of superoxide, nitric oxide, and hydrogen peroxide were all reduced in the arthritic joints. |
References: | |
Chemical Properties
CAS No.
163847-77-6
Synonyms
TAPI
Chemical Name
N1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide
SMILES
NCCNC([C@@H](C)NC([C@H](NC(C(CC(C)C)CC(NO)=O)=O)CC1=CC2=CC=CC=C2C=C1)=O)=O
Molecular Formula
C26H37N5O5
Molecular Weight
499.6
Solubility
≥ 24.98mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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