TAPI-2

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Chemical Structure| 187034-31-7 同义名 : TNF Protease Inhibitor 2
CAS号 : 187034-31-7
货号 : A441461
分子式 : C19H37N5O5
纯度 : 99%+
分子量 : 415.53
MDL号 : N/A
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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

[1]Wang R, Ye X, 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.

[2]Kruse MN, Becker C, 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.