1. Metabolic Enzyme/Protease
  2. MMP

TAPI-2 

Cat. No.: HY-100211 Purity: 95.93%
Handling Instructions

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 μM for MMP.

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
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 720 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 1140 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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 μM for MMP.

IC50 & Target

IC50: 20±10 μM (MMP)[1] Ki: 1.5±0.27 nM (MMPs)[1]

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)[2].

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
Kinase Assay
[1]

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].

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

Cell Assay
[2]

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].

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

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
TAPI-2
Cat. No.:
HY-100211
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TAPI-2

Cat. No.: HY-100211