TAPI-1

Catalog No.S7434 Batch:S743401

Technical Data

Formula	C₂₆H₃₇N₅O₅
Molecular Weight	499.60	CAS No.	171235-71-5
Solubility (25°C)*	In vitro	DMSO	99 mg/mL (198.15 mM)
		Ethanol	99 mg/mL (198.15 mM)
		Water	60 mg/mL (120.09 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

In vivo

TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors

Protocol (from reference)

Cell Assay:^{^[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.
Animal Study:^{^[6]}	Animal Models Male Sprague-Dawley rats Dosages 1 μg Administration i.c.v.

Cell Assay:^{^[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.

Animal Study:^{^[6]}

Animal Models
Male Sprague-Dawley rats
Dosages
1 μg
Administration
i.c.v.

References

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Customer Product Validation

: Data from [Data independently produced by , , Sci Rep, 2017, 7:46315]

: Data from [Data independently produced by , , Biochim Biophys Acta Gen Subj, 2018, 1862(9):1988-1994]

Selleck's TAPI-1 has been cited by 25 publications

Immune evasion in lung metastasis of leiomyosarcoma: upregulation of EPCAM inhibits CD8+ T cell infiltration [ Br J Cancer, 2024, 10.1038/s41416-024-02576-z]	PubMed: 38291183
Semaphorin 7A promotes endothelial permeability and inflammation via plexin C1 and integrin β1 in Kawasaki disease [ BMC Pediatr, 2024, 24(1):285]	PubMed: 38678170
Multiplex interrogation of the NK cell signalome reveals global downregulation of CD16 signaling during lentivirus infection through an IL-18/ADAM17-dependent mechanism [ PLoS Pathog, 2023, 19(9):e1011629]	PubMed: 37669308
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530]	PubMed: 37543570
Epithelial cell adhesion molecule (EpCAM) regulates HGFR signaling to promote colon cancer progression and metastasis [ J Transl Med, 2023, 21(1):530]	PubMed: 37543570
Multiplex interrogation of the NK cell signalome reveals global downregulation of CD16 signaling during lentivirus infection through an IL-18/ADAM17-dependent mechanism [ PLoS Pathog, 2023, 19(9):e1011629]	PubMed: 37669308
MiR-92a/KLF4/p110δ regulates titanium particles-induced macrophages inflammation and osteolysis [ Cell Death Discov, 2022, 8(1):197]	PubMed: 35418181
The collectrin-like part of the SARS-CoV-1 and -2 receptor ACE2 is shed by the metalloproteinases ADAM10 and ADAM17 [ FASEB J, 2022, 36(3):e22234]	PubMed: 35199397
Targeting the EGFR-ERK axis using the compatible solute ectoine to stabilize CFTR mutant F508del [ FASEB J, 2022, 36(5):e22270]	PubMed: 35412656
Complete abrogation of key osteoclast markers with a membrane-anchored tissue inhibitor of metalloproteinase : a novel approach in the prevention of osteoclastogenesis [ Bone Joint Res, 2022, 11(11):763-776]	PubMed: 36331083

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.