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NSC 405020
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NSC 405020图片
CAS NO:7497-07-6
规格:98%
分子量:260.16
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
MT1-MMP inhibitor
CAS:7497-07-6
分子式:C12H15Cl2NO
分子量:260.16
纯度:98%
存储:Store at -20°C

Background:

NSC-405020 is a novel small molecule inhibitor of membrane type-I matrix metalloproteinase (MT1-MMP) that specifically targets the hemopexin (PEX) domain rather than the catalytic domain of MT1-MMP with 50% inhibition concentration IC50value larger than 100 μmol/L and does not inhibit the catalytic activity of MT1-MMP or MMP-2. NSC-405020 directly interacts with and binds to PEX in a vicinity of Met-328, Arg-330, Asp-376, Met-22 and Ser-470 of the druggable pocket in the full-length MT1-MMP structure, which affects the conformation and flexibility of blades I to IV of the β-propeller resulting in the decrease of the PEX-dependent homodimerization of cellular MT1-MMP. NSC-405020 dose not affect the ability of MT1-MMP to activate MMP-2 but its ability to degrade COL-I.


Reference


[1].Remacle AG, Golubkov VS, Shiryaev SA, Dahl R, Stebbins JL, Chernov AV, Cheltsov AV, Pellecchia M, Strongin AY. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012 May 1;72(9):2339-49. doi: 10.1158/0008-5472.CAN-11-4149. Epub 2012 Mar 9.