生物活性 | |||
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描述 | 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]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.03mL 2.41mL 1.20mL |
24.07mL 4.81mL 2.41mL |
参考文献 |
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