TAPI-2 is a broad-spectrum inhibitor of MMP (IC50: 20 μM), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM).

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].

187034-31-7

C19H37N5O5

415.53

TAPI-2

DMSO:20 mg/mL (48.13 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years