TAPI-1

Catalog No.S7434

For research use only.

TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. TAPI-1 is also an inhibitor of Matrix Metalloproteinase (MMP).

TAPI-1 Chemical Structure

CAS No. 171235-71-5

Selleck's TAPI-1 has been cited by 17 publications

Purity & Quality Control

Choose Selective Immunology & Inflammation related Inhibitors

Biological Activity

Description TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. TAPI-1 is also an inhibitor of Matrix Metalloproteinase (MMP).
Targets
ADAM17/TACE [1] MMP [5]
In vitro

TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. [1] TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). [2] TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. [3] TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells. [4]

Assay
Methods Test Index PMID
Western blot p-EGFR(Y1068) / EGFR / p-AKT / AKT / p-ERK / ERK 31426531

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: LI90 cells
  • Concentrations: 20 μM
  • Incubation Time: 60 hours
  • Method:

    Five thousand cells are seeded into each well of 96-well plates and their viability is assessed by CellTiter-Glo Luminescent Cell Viability assay. Upon serum deprivation for 24 h, the cells are treated with Ang II for 60 h with and without pretreatment with each inhibitor and antagonist. The assay substrates are then added to each well on the plate and the samples are evaluated using a luminometer.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 499.60
Formula

C26H37N5O5

CAS No. 171235-71-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CC2=CC=CC=C2C=C1)C(=O)NC(C)C(=O)NCCN

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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