| Description | TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. |
| 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. 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. |
| molecular weight | 613.62 |
| Molecular formula | C28H38F3N5O7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10 mM |
| References | 1. Müllberg J, et al. J Immunol. 1995, 155(11), 5198-5205 2. Slack BE, et al. Biochem J. 2001, 357(Pt 3), 787-794. 3. Oikawa H, et al. Life Sci. 2014, 97(2), 137-144. |