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TAPI-2 (TAPI2) is a novel and potent inhibitor of matrix metalloproteinases (MMPs, IC50 = 20±10 μM), disintegrin and metalloproteinase (ADAM), and tumor necrosis factor-α converting enzyme (TACE).
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| ln Vitro |
The hydroxamate-based metalloproteinase inhibitor TAPI-2 binds to hmeprin; its inhibitory constants (IC50) are 20±10 μM for the hmeprin β subunit and 1.5±0.27 nM for the hmeprin α subunit, respectively. Generally speaking, the α subunit exhibits stronger inhibition than the β subunit [1]. Without changing the expression of ADAM17, TAPI-2 dramatically lowered the protein levels of NICD and its downstream target HES-1 in HCP-1 and HT29 cells. Additionally, TAPI-2 treatment of the cells markedly decreased the CSC phenotype in both CRC cell lines by -50%. The established dose range of TAPI-2 (5-40 μM) was not exceeded by the concentration employed (20 μM), as demonstrated by the dose-dependent effects of TAPI-2 on spheroid formation and protein levels of NICD and HES-1 [3].
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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.
[2]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [3]. 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 |
| Molecular Formula |
C19H37N5O5
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|---|---|
| Molecular Weight |
415.5276
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| CAS # |
187034-31-7
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| Related CAS # |
(R)-TAPI-2;689284-12-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(C([H])(C([H])([H])C(N([H])O[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])[C@]([H])(C(N([H])C([H])(C(N([H])C([H])([H])C([H])([H])N([H])[H])=O)C([H])([H])[H])=O)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~240.66 mM)
Ethanol : ~50 mg/mL (~120.33 mM) DMSO : ≥ 22 mg/mL (~52.94 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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