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 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.

Research Areas >> Cancer

[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.

GM 6001 | T-5224 | SB-3CT | Batimastat | Astragaloside IV | Marimastat (BB-2516) | edaravone | TAPI-2 | TAPI 1 | ISOGINKGETIN | Arctigenin | CTS-1027 | GI254023X | JNJ 0966 | CL-82198