CS-2628

中文名称:

CS-2628

中文同义词:

MMP/TACE和ADAM抑制剂(TAPI-2)

英文名称:

TAPI-2

英文同义词:

TAPI-2;N-(R)-[2-(HYDROXYAMINOCARBONYL)METHYL]-4-METHYLPENTANOYL-L-T-BUTYL-ALANYL-L-ALANINE, 2-AMINOETHYL AMIDE;N-(R)-(2-(HYDROXYAMINOCARBONYL)METHYL)-4-METHYLPENTANOYL-L-T-BUTYL-GLYCYL-L-ALANINE 2-AMINOETHYL AMIDE;TNF-ALPHA PROTEASE INHIBITOR-2;HONHCOCH2CH(CH2-CH(CH3)2)CO-T-LEU-ALA-NHCH2CH2NH2;N-[2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-methyl-L-valyl-N-(2-aminoethyl)-L-alaninamide;N-[2-[2-(HydroxyaMino)-2-oxoethyl]-4-Methyl-1-oxopentyl]-3-Methyl-L-valyl-N-(2-aMinoethyl)-L-alaninaMide Acetic Acid;TAPI-2 (TNF Protease Inhibitor 2)

CAS号:

187034-31-7

分子式:

C19H37N5O5

分子量:

415.53

EINECS号:

相关类别:

细胞生物学试剂;A hydroxamate-based inhibitor of MMPs and TACE.

Mol文件:

Mol File

敏感性 

Light Sensitive Hygroscopic

生物活性

TAPI-2 (TNF Protease Inhibitor 2) 是基质金属蛋白酶 (MMP)，肿瘤坏死因子α 转换酶 (TACE) 和解联蛋白和金属蛋白酶 (ADAM) 的广谱抑制剂, 对 MMP 的IC50 值为 20 μM。TAPI-2 阻止传染性 SARS-CoV 进入。

靶点

MMP 20 μM (IC 50 )

MMP 20 μM (IC 50 )

体外研究

The hydroxamate-based metalloprotease inhibitor TAPI-2 bounds to hmeprin with inhibition constants IC 50 20±10 μM for hmeprin β subunit and 1.5±0.27 nM for hmeprin α subunit. Generally, hmeprin α is inhibited more strongly than the β subunit. 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).