TAPI-2 (Synonyms: TNF Protease Inhibitor 2) |
Catalog No.GC19347 |
TAPI-2 (TNF Protease Inhibitor 2) est un inhibiteur À large spectre de la métalloprotéase matricielle (MMP), de l'enzyme de conversion du facteur de nécrose tumorale (TACE) et d'une désintégrine et métalloprotéinase (ADAM), avec une IC50 de 20 μM pour la MMP. TAPI-2 bloque l'entrée du SRAS-CoV infectieux.
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Cas No.: 187034-31-7
Sample solution is provided at 25 µL, 10mM.
TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20±10 uM for MMP.
The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC50 20±10 uM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit. Generally, hmeprin α is inhibited more strongly than the β subunit[1]. Without affecting ADAM17 expression, TAPI-2 dramatically decreases the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells. Moreover, treating cells with TAPI-2 significantly decreases the CSC phenotype by -50% in both CRC cell lines. The dose-dependent effects of TAPI-2 on the sphere formation and protein levels of NICD and HES-1 confirm that the concentration used (20 uM) is within the effective dose range of TAPI-2 (5-40 uM)[2].
References:
[1]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9.
[2]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8.
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