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TAPI-2

Cat. No. M6216
TAPI-2 Structure
Size Price Availability Quantity
1mg USD 190 In stock
5mg USD 670 In stock
10mg USD 1050 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. 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).

Protocol
Cell Experiment
Cell lines HEK293T cells
Preparation method 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.
Concentrations 20 μM
Incubation time 48 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 415.53
Formula C19H37N5O5
CAS Number 187034-31-7
Purity >98%
Solubility 22 mg/mL in DMSO
Storage at -20°C
References

Enhanced potency of the metalloprotease inhibitor TAPI-2 by multivalent display.
Raissi AJ, et al. Bioorg Med Chem Lett. 2014 Apr 15;24(8):2002-7. PMID: 24581919.

Cyclosporin A and tacrolimus induce renal Erk1/2 pathway via ROS-induced and metalloproteinase-dependent EGF-receptor signaling.
Akool el-S, et al. Biochem Pharmacol. 2012 Jan 15;83(2):286-95. PMID: 22100870.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAPI-2 supplier, inhibitors

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