| Description | TAPI1 (TAPI) , an ADAM17/TACE inhibitor, inhibits shedding of cytokine receptors. |
| In vitro | TAPI-1 能够阻止未激活及PMA诱导的THP-1单核细胞系及人体外周血单核细胞可溶性TNF-alpha、p60 TNFR和IL-6R的释放。此外，TAPI-1 还能抑制LPS诱导的p60 TNFR和TNF-alpha在单核细胞中的脱落。[1] TAPI-1 抑制了TACE依赖的APP(695)共转染产物的持续释放。[2] TAPI-1 减弱了Ang II诱导的人体HSC系LI90的EGFR转激活和细胞增殖。[3] 结合EGFR抑制剂AG1478，TAPI-1 能够使AREG/EGFR/ERK信号通路失活，并在pSS唾液腺来源上皮细胞中减少促炎细胞因子的释放。[4] |
| Cell experiments | 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) |
| Synonyms | TAPI 1, TAPI, TAPI-1 |
| molecular weight | 499.612 |
| Molecular formula | C26H37N5O5 |
| CAS | 163847-77-6 |
| Storage | store at low temperature,keep away from moisture|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 92 mg/mL (184.1 mM) H2O: 55 mg/mL (110.1 mM) DMSO: 92 mg/mL (184.1 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. 4. Sisto M, et al. 2014. DOI 10.12007/s10238-2014-0279-4. |