| Description | TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM). |
| In vitro | TAPI-2 bounds to h-meprin with IC50 20 μM for h-meprin β subunit and 1.5 nM for h-meprin α subunit. Generally, h-meprin 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 μM) is within the effective dose range of TAPI-2 (5–40 μM) [2]. |
| Target activity | MMP:20 μM, MMP:1.5 nM (Ki) |
| Synonyms | TAPI-2 |
| molecular weight | 415.53 |
| Molecular formula | C19H37N5O5 |
| CAS | 187034-31-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 20 mg/mL (48.13 mM) |
| 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. |