TAPI-1 (Synonyms: TAPI) |
Katalog-Nr.GC12344
One-Click Copy Product Info
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TAPI-1 ist ein TACE (ADAM17)-Inhibitor und blockiert die Freisetzung mehrerer ZelloberflÄchenproteine.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 163847-77-6
Sample solution is provided at 25 µL, 10mM.
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.
| 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: | |
| Cas No. | 163847-77-6 | SDF | |
| Überlieferungen | 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 | ||
| Canonical 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 | ||
| Formula | C26H37N5O5 | M.Wt | 499.6 |
| Löslichkeit | ≥ 24.98mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0016 mL | 10.008 mL | 20.016 mL |
| 5 mM | 400.3 μL | 2.0016 mL | 4.0032 mL |
| 10 mM | 200.2 μL | 1.0008 mL | 2.0016 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)