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.
CAS：187034-31-7
分子式：C19H37N5O5
分子量：415.53
纯度：98%
存储：Store at -20°C

Background:

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].

参考文献:
[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.