Product Data SheetProduct Name:CAS No.: CatNo:Cat. No.:MWt:Formula:Purity :TAPI-1163847-77-6HY-16657HY16657499.60C26H37N5O5>98%Solubility:DMSOMechanisms: Pathways:Others; Target:Others Biological Activity: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 MUC5ACmucin production, whereas TGF-α-neutralizing antibody, but not AR- or HB-EGF-neutralizingantibody, inhibited LL-37-induced EGFR activation and subsequent MUC5AC mucin production inNCI-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 andisolatedkeratinocytes[2]PretreatmentwithantibodyagainstFcγRII or with CD32 siRNA, p47(phox)isolated keratinocytes [2]. Pretreatment with antibody against FcRIIorwithCD32siRNAp47(phox)siRNA, apocynin, N-acetylcysteine, tumor necrosis factor-α protease inhibitor 1 (TAPI-1) or TACEsiRNA attenuated sLOX-1 release induced by CRP. CRP also elevated serum sLOX-1 levels in arabbit model of atherosclerosis [3]....References:[1]. Zhang Y, et al. The human Cathelicidin LL-37 induces MUC5AC mucin production by airwayepithelial cells via TACE-TGF-α-EGFR pathway. Exp Lung Res. 2014 Jun 5. [2]. Wheeler DL, et al. Protein kinase Cepsilon is linked to 12-O-tetradecanoylphorbol-13-acetate-idinduced tumor necrosis factor-alpha ectodomain shedding and the development of metastaticdtiftlhtdihddidthdltftttisquamous cell carcinoma in protein kinase Cepsilon transgenic mice. Cancer Res. 2003 Oct1;63(19):6547-55. [3]. Zhao XQ, et al. CRP enhances soluble LOX-1 release from macrophages by activating TNF-αconverting enzyme. J Lipid Res. 2011 May;52(5):923-33. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
