tcsc3108 TAPI-1

TAPI-1 is a specific TACE (TNF-α-converting enzyme) inhibitor.

IC50 value:

Target:

TAPI-1 inhibited LL-37-induced TGF-α production, EGFR activation and subsequent MUC5AC mucin production, whereas TGF-α-neutralizing antibody, but not AR- or HB-EGF-neutralizing antibody, inhibited LL-37-induced EGFR activation and subsequent MUC5AC mucin production in NCI-H292 cells [1]. Using the TNF-alpha converting enzyme (TACE) inhibitor, TAPI-1, TPA-stimulated TNFalpha shedding could be completely prevented in PKCepsilon transgenic mice and isolated keratinocytes [2]. Pretreatment with antibody against FcγRII or with CD32 siRNA, p47(phox) siRNA, apocynin, N-acetylcysteine, tumor necrosis factor-α protease inhibitor 1 (TAPI-1) or TACE siRNA attenuated sLOX-1 release induced by CRP. CRP also elevated serum sLOX-1 levels in a rabbit model of atherosclerosis [3].