1. Metabolic Enzyme/Protease
    Anti-infection
  2. MMP
    SARS-CoV
  3. TAPI-2

TAPI-2 (Synonyms: TNF Protease Inhibitor 2)

Cat. No.: HY-100211 Purity: >95.0%
Handling Instructions

TAPI-2 (TNF Protease Inhibitor 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 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.

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

TAPI-2 Chemical Structure

TAPI-2 Chemical Structure

CAS No. : 187034-31-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 658 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 720 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

TAPI-2 (TNF Protease Inhibitor 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 μM for MMP[1]. TAPI-2 blocks the entry of infectious SARS-CoV[2].

IC50 & Target[1]

MMP

20 μM (IC50)

In Vitro

The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC50 20±10 μM 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 μM) is within the effective dose range of TAPI-2 (5-40 μM)[3].

Molecular Weight

415.53

Formula

C₁₉H₃₇N₅O₅

CAS No.

187034-31-7

SMILES

CC(C)(C)[[email protected]@H](C(N[[email protected]](C(NCCN)=O)C)=O)NC(C(CC(NO)=O)CC(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 22 mg/mL (52.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

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[3].

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

References
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Keywords:

TAPI-2TNF Protease Inhibitor 2TAPI2TAPI 2TNF Protease Inhibitor2TNF Protease Inhibitor-2MMPSARS-CoVMatrix metalloproteinasesSARS coronavirusInhibitorinhibitorinhibit

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TAPI-2
Cat. No.:
HY-100211
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