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MMP-9-IN-1

Names

[ CAS No. ]:
502887-71-0

[ Name ]:
MMP-9-IN-1

Biological Activity

[Description]:

MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[Target]

MMP-9


[In Vitro]

MMP-9-IN-1 (compound 2; 100 μM; 14 hours) does not cause notable cytotoxicity[1]. MMP-9-IN-1 (compound 2; 10 μM) significantly inhibits cell proliferation of HT-1080 and MDA-MB-435 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: COS-1 monkey epithelial cell lines Concentration: 100 μM Incubation Time: 24 hours Result: Treatment did not cause notable cytotoxicity. Cell Proliferation Assay[1] Cell Line: HT-1080 and MDA-MB-435 cancer cells expressing endogenous MMP-9 Concentration: 10 μM Incubation Time: 9 days Result: Significant inhibition of cell proliferation.

[In Vivo]

MMP-9-IN-1 (compound 2; 20 mg/kg; intraperitoneal and intratumoral injection alternately; 6 days/week; for 14 weeks) results in a profound delay in tumor growth in NCR-Nu mice bearing MDA-MB-435/GFP tumor[1]. MMP-9-IN-1 inhibits cancer cell metastasis in vivo[1]. Animal Model: 4-5 week-old female NCR-Nu mice bearing MDA-MB-435/GFP tumor[1] Dosage: 20 mg/kg Administration: Intraperitoneal and intratumoral injection alternately; 6 days/week; for 14 weeks, Result: Resulted in a profound delay in tumor growth. Inhibited cancer cell metastasis.

[References]

[1]. Dufour A, et al. Small-molecule anticancer compounds selectively target the hemopexin domain of matrix metalloproteinase-9. Cancer Res. 2011 Jul 15;71(14):4977-88.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H17F2N3O3S

[ Molecular Weight ]:
369.39


Related Compounds