product name TAPI-1
Description: TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. Specifically, it catalyzes the cleavage of full-length APP to the soluble N-terminal fragment (sAPPα). The release of sAPPα has been reported to be a receptor-coupled process increased by the stimulation of muscarinic receptors. In HEK293 cells, treatment of TAPI-1 resulted in an inhibition of increased sAPPα which was induced by the expressing of M3 subtype. The IC50 values of TAPI-1 in the inhibition of M3-increased sAPPα and constitutive release of sAPPα were 3.61 μM and 8.09 μM, respectively.
References: J Immunol. 1995 Dec 1;155(11):5198-205; Biochem J. 2001 Aug 1;357(Pt 3):787-94; Life Sci. 2014 Mar 3;97(2):137-44.
499.60
Formula
C26H37N5O5
CAS No.
171235-71-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (198.2 mM)
Water: 60 mg/mL (120.1 mM)
Ethanol: 99 mg/mL (198.2 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. 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. Kinase Assay: Cell Assay: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Immunol. 1995 Dec 1;155(11):5198-205; Biochem J. 2001 Aug 1;357(Pt 3):787-94; Life Sci. 2014 Mar 3;97(2):137-44. |
