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Product Feature - MMP Inhibitors
Degradation of the extracellular matrix (ECM) is an important process in tissue remodeling, repair and morphogenesis. Matrix metalloproteinases (MMPs), also called matrixins, are zinc-dependent endopeptidases that are the major proteases involved in ECM degradation. MMPs play a central role in cell proliferation, migration, differentiation, angiogenesis, apoptosis and host defences. Their dysregulation has been implicated in many diseases including arthritis, chronic ulcers, encephalomyelitis and cancer.
Key MMP inhibitors now available from Tocris include:
Broad spectrum MMP inhibitor
2631 l Marimastat An orally available and potent inhibitor of most of the major MMPs. In vivo, inhibits tumour angiogenesis in the SCID/human gastric cancer model of peritoneal dissemination. Related Product: PD 166793
Selective inhibitor of MMP-2
2621 l ARP 100 Displays selectivity over MMP-9, MMP-3, MMP-1 and MMP-7. Exhibits anti-invasive properties in an in vitro model using fibrosarcoma HT1080 cells, a cell line that overexpresses MMP-2 and MMP-9. Related Product: ARP 101
Potent and selective inhibitor of MMP-13
2633 l WAY 170523 IC50 values are 17, 945, > 1000 and > 10000 nM for MMP-13, MMP-9, TACE and MMP-1 respectively. Related Product: CL 82198
View all ECM-Related Products.
MMPs in Cancer
Tumour metastasis is a multistep process involving the dissemination of tumour cells from the primary tumour to secondary tumours at a distant organ or tissue. One of the first steps in metastasis is the degradation of the basement membrane, a process in which MMPs have been implicated. MMPs are secreted by tumour cells themselves or by surrounding stromal cells stimulated by the nearby tumour. Numerous studies have linked altered MMP expression in different human cancers with poor prognosis. MMP-1, -2, -3, -7, -9, -13 and -14 all have elevated expression in primary tumours and/or metastases. Synthetic or natural inhibitors of MMPs result in inhibition of metastasis, while up-regulation of MMPs lead to enhanced cancer cell invasion.
For more information request our Guide to Cancer Research.
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