TAPI-2 (Synonyms: TNF Protease Inhibitor 2) |
| رقم الكتالوجGC19347 |
TAPI-2 (TNF Protease Inhibitor 2) هو مثبط واسع الطيف لمصفوفة metalloprotease (MMP) ، إنزيم تحويل عامل نخر الورم (TACE) و disintegrin و metalloproteinase (ADAM) ، مع IC 50 من 20 ميكرومتر لـ MMPيمنع TAPI-2 دخول فيروس السارس المعدي
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Cas No.: 187034-31-7
Sample solution is provided at 25 µL, 10mM.
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TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20±10 uM for MMP.
The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC50 20±10 uM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit. Generally, hmeprin α is inhibited more strongly than the β subunit[1]. Without affecting ADAM17 expression, TAPI-2 dramatically decreases the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells. Moreover, treating cells with TAPI-2 significantly decreases the CSC phenotype by -50% in both CRC cell lines. The dose-dependent effects of TAPI-2 on the sphere formation and protein levels of NICD and HES-1 confirm that the concentration used (20 uM) is within the effective dose range of TAPI-2 (5-40 uM)[2].
References:
[1]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9.
[2]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8.
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Kinase experiment: |
Meprin activities are determined using N-benzoyl-L-tyrosyl p-aminobenzoic acid as substrate. The substrate concentration is 40 mM, and the enzyme concentration is always at least 10 times below Ki. Inhibitors are employed in a concentration range from 5 pM to 5 mM, depending on their inhibitory effect. Each inhibitor is tested over a concentration range covering at least ten different concentrations from Ki/5 to 5×Ki. All reactions are carried out at 37°C in 50 mM Tris/HCl, pH 7.5, and 0.5 mM MgCl2[1]. |
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Cell experiment: |
TAPI-2 is dissolved in DMSO and diluted with appropriate medium before use. All experiments are performed using 20 μM TAPI-2. Cells are cultured with or without TAPI-2 for 48 hours and then seeded at 3,000 cells per well in 96-well plates. After pretreatment, increasing doses of 5-fluorouracil (5-FU) that are relevant to the recommended clinical dose (up to 2 μg/mL) are added, with or without TAPI-2, for 72 hours. Cell viability is assessed by adding MTT substrate (0.25% in phosphate-buffered saline [PBS]) in growth medium (1:5 dilution) to cells for 1 hour at 37°C. The cells are ished with PBS, and 100 μL of dimethyl sulfoxideis added. Optical density is measured at 570 nM, and relative MTT is presented as a percentage of control[2]. |
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References: [1]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. |
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| Cas No. | 187034-31-7 | SDF | |
| المرادفات | TNF Protease Inhibitor 2 | ||
| Canonical SMILES | CC(C)(C)[C@@H](C(N[C@H](C(NCCN)=O)C)=O)NC(C(CC(NO)=O)CC(C)C)=O | ||
| Formula | C19H37N5O5 | M.Wt | 415.53 |
| الذوبان | DMSO : ≥ 22 mg/mL (52.94 mM) | 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 | 2.4066 mL | 12.0328 mL | 24.0657 mL |
| 5 mM | 0.4813 mL | 2.4066 mL | 4.8131 mL |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4066 mL |
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- Purity: >99.00%
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