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 μM for MMP.
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International
TAPI-2, known as TNF Protease Inhibitor 2, is a comprehensive inhibitor that targets matrix metalloprotease (MMP), tumor necrosis factorα-converting enzyme (TACE), and a disintegrin and metalloproteinase (ADAM), with an IC50 value of 20 μM for MMP[1]. TAPI-2, a hydroxamate-based metalloprotease inhibitor, binds to hmeprin and exhibits inhibition constants with an IC50 of 20±10 μM for the hmeprin β subunit and 1.5±0.27 nM for the hmeprin α subunit. Typically, the hmeprin α subunit is more strongly inhibited than the β subunit[2]. TAPI-2 does not alter ADAM17 expression but significantly reduces the protein levels of NICD and its downstream target HES-1 in both HCP-1 and HT29 cells. Additionally, TAPI-2 treatment markedly diminishes the CSC phenotype by 50% in both CRC cell lines. The observed dose-dependent impact of TAPI-2 on sphere formation and the protein levels of NICD and HES-1 validates that the utilized concentration of 20 μM is within the effective dosage range for TAPI-2, which spans 5-40 μM[3].
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