NSC 405020 (Synonyms: NSC405020, NSC-405020) |
| Catalog No.GC14210 |
N/A
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 7497/7/6
Sample solution is provided at 25 µL, 10mM.
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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 IC50 value 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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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