Home Immunology & Inflammation Immunology & Inflammation related inhibitor - MMP inhibitor TAPI-1 For research use only.

TAPI-1

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

TAPI-1 Chemical Structure

CAS: 171235-71-5

Selleck's TAPI-1 has been cited by 22 Publications

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Purity & Quality Control

Batch: Purity: 99.35%
99.35

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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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-EGFR(Y1068) / EGFR / p-AKT / AKT / p-ERK / ERK 31426531
In Vivo
In vivo

TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 1 μg
Administration i.c.v.

Chemical Information & Solubility

Molecular Weight 499.60 Formula

C26H37N5O5
CAS No. 171235-71-5 SDF Download TAPI-1 SDF
Smiles CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CC2=CC=CC=C2C=C1)C(=O)NC(C)C(=O)NCCN
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (198.15 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 99 mg/mL

Ethanol : 99 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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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