NSC 405020

CAS No. : 7497-07-6

NSC 405020,7497-07-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000060
Molecular Formula:C₁₂H₁₅Cl₂NO
Molecular Weight:260.16
IC50:> 100 uM [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000060
Cas No:7497-07-6
Product-Name:NSC 405020

NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
IC50 value: > 100 uM [1]
Target: MT1-MMP PEX inhibitor
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.

[1]. Remacle AG, et al. 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.

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