TAPI1 (TAPI) , an ADAM17/TACE inhibitor, inhibits shedding of cytokine receptors.

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]

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. (Only for Reference)