7497-07-6

7497-07-6 structure

Name: NSC 405020
Chemical Name: 3,4-dichloro-N-pentan-2-ylbenzamide
CAS Number: 7497-07-6
Molecular Formula: C₁₂H₁₅Cl₂NO
Molecular Weight: 260.160
Catalog: Biochemical Inhibitor Proteases MMP inhibitor
Create Date: 2017-05-01 12:44:53
Modify Date: 2024-01-03 21:45:03
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 inhibitorNSC-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.

Name	3,4-dichloro-N-pentan-2-ylbenzamide
Synonyms	3,4-Dichloro-N-(2-pentanyl)benzamide Benzamide, 3,4-dichloro-N-(1-methylbutyl)- NSC 405020

Description	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 inhibitorNSC-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.
Related Catalog	Research Areas >> Cancer
References	[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.